Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade

ABSTRACT

The invention relates to polycyclic aryl and heteroaryl substituted benzene compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

FIELD OF THE INVENTION

[0001] This invention is in the field of anticoagulant therapy, andspecifically relates to compounds, compositions and methods forpreventing and treating thrombotic conditions such as coronary arteryand cerebrovascular disease. More particularly, the invention relates topolycyclic aryl and heteroaryl substituted benzene compounds thatinhibit serine proteases of the coagulation cascade.

BACKGROUND OF THE INVENTION

[0002] Physiological systems control the fluidity of blood in mammals[Majerus, P. W. et al: Anticoagulant, Thrombolytic, and AntiplateletDrugs. In Hardman, J. G. and Limbird, L. E., editors: Goodman & Gilman'sThe Pharmacological Basis of Therapeutics. 9th edition. New York,McGraw-Hill Book Co., 1996, pp. 1341-1343]. Blood must remain fluidwithin the vascular systems and yet be able to undergo hemostasis,cessation of blood loss from a damaged vessel, quickly. Hemostasis orclotting begins when platelets first adhere to macromolecules insubendothelian regions of an injured and/or damaged vessels. Theseplatelets aggregate to form the primary hemostatic plug and stimulatelocal activation of plasma coagulation factors leading to generation ofa fibrin clot that reinforces the aggregated platelets.

[0003] Plasma coagulation factors include factors II, V, VII, VIII, IX,X, XI, and XII; these are also called protease zymogens. Thesecoagulation factors or protease zymogens are activated by serineproteases leading to coagulation in a so called “coagulation cascade” orchain reaction [Handin, R. I.: Bleeding and Thrombosis. In Wilson, J.,et al. editors: Harrison's Principles of Internal Medicine. 12thEdition, New York, McGraw-Hill Book Co., 1991,p.350]. Coagulation orclotting occurs in two ways through different pathways. An intrinsic orcontact pathway leads from XII to XIIa to XIa to IXa and to theconversion of X to Xa. Xa with factor Va converts prothrombin (II) tothrombin (IIa) leading to conversion of fibrinogen to fibrin.Polymerization of fibrin leads to a fibrin clot. An extrinsic pathway isinitiated by the conversion of coagulation factor VII to VIIa by Xa. Thepresence of Tissue Factor and VIIa accelerates formation of Xa in thepresence of calcium ion and phospholipids. Formation of Xa leads tothrombin, fibrin, and a fibrin clot as described above. The presence ofone or more of these many different coagulation factors and two distinctpathways of clotting could enable the efficacious, selective control andbetter understanding of parts of the coagulation or clotting process.

[0004] While clotting as a result of an injury to a blood vessel is acritical physiological process for mammals such as man, clotting canalso lead to disease states. A pathological process called thrombosisresults when platelet aggregation and/or a fibrin clot blocks (i.e.,occludes) a blood vessel. Arterial thrombosis may result in ischemicnecrosis of the tissue supplied by the artery. When the thrombosisoccurs in a coronary artery, a myocardial infarction or heart attack canresult. A thrombosis occurring in a vein may cause tissues drained bythe vein to become edematous and inflamed. Thrombosis of a deep vein maybe complicated by a pulmonary embolism. Preventing or treating clots ina blood vessel may be therapeutically useful by inhibiting formation ofblood platelet aggregates, inhibiting formation of fibrin, inhibitingthrombus formation, inhibiting embolus formation, and for treating orpreventing unstable angina, refractory angina, myocardial infarction,transient ischemic attacks, atrial fibrillation, thrombotic stroke,embolic stroke, deep vein thrombosis, disseminated intravascularcoagulation, ocular build up of fibrin, and reocclusion or restenosis ofrecanalized vessels.

[0005] There have been several reports of non-peptidic benzene compoundsthat act as an inhibitor of a coagulation factor present in thecoagulation cascade or clotting process. In PCT. Patent Applications WO99/00121 and WO 99/00128, Beight et al. describe certain aroylamido,aroyloxy, and N-arylamidocarbonyl and certain heteroaroylamido,heteroaroyloxy, and N-heteroarylamidocarbonyl benzenes that may befurther substituted at the other benzene ring carbons by other groupsand that are reported to have inhibitory activity against factor Xa. InU.S. Pat. No. 5,872,138 and PCT Patent Application WO 98/10763,Naylor-Olsen et al. describe disubstituted benzenes having a grouplinked through an oxygen, nitrogen or sulfur heteroatom, any one of sixbasic heterocycles linked to the ring through linker group, and,optionally, an additional alkyl, alkenyl, alkoxy, amino, orarylmethylenesulfonamido group and claimed to inhibit human thrombin. InPCT Patent Application WO 99/26920, Semple et al. disclose1-oxy-2,3,4,5-tetrasubstituted-phenylacetamides having an acyl functionin the group substituting the amide nitrogen and having activity againstthrombin. In PCT Patent Application WO 96/39380, Lu and Soll describebis-(sulfonamido substitutedbenzoyl) derivatives of diamines claimed tohave utility as inhibitors of thrombotic disorders. In PCT PatentApplication WO 96/40100, Illig et al. describe sulfonamidosubstitutedbenzoyl and benzyl derivatives of amines directed tonon-peptidic factor Xa and claimed to have utility as inhibitors ofthrombotic disorders. In PCT Patent Applications WO 00/039102, Wexler etal. describe certain 3-(amino substituted bicvclic heteroaryl)-propoxy,-propylamino, and -propanoylamido benzene compounds that may be furthersubstituted at the other two benzene ring carbons by other groups andthat are reported to be inhibitors of trysin-like serine proteaseenzymes, especially factor Xa and thrombin.

SUMMARY OF THE INVENTION

[0006] It is an object of the present invention to provide novelcompounds that are beneficial in anticoagulant therapy and that have ageneral structure:

[0007] It is another object of the present invention to provide methodsfor preventing and treating thrombotic conditions, such as coronaryartery disease, cerebrovascular disease, and other coagulation relateddisorders. Such thrombotic conditions are prevented and treated byadministering to a patient in need thereof an effective amount ofcompounds of Formula (I).

[0008] Various other objects and advantages of the present inventionwill become apparent from the following description of the invention.

DESCRIPTION OF THE INVENTION

[0009] The present invention relates to a class of compounds comprisingPolycyclic Aryl and Heteroaryl Substituted Benzenes, which arebeneficial in anticoagulant therapy for the treatment and prevention ofa Variety of thrombotic conditions including coronary artery andcerebrovascular disease, as given in Formula (I):

[0010] or a pharmaceutically acceptable salt thereof, wherein;

[0011] J is selected from the group consisting of hydrido, halo,hydroxy, hydroxyalkyl, amino, aminoalkyl, cyano, alkyl, alkenyl,haloalkyl, haloalkenyl, carboxy, carboxyalkyl, carboalkoxy,amidocarbonyl, acyl, phosphono, sulfo, O—R⁶, NH—R⁶, S—R⁶, S(O)—R⁶, andS(O)₂—R⁶, wherein R⁶ is selected from the group consisting of alkyl,alkenyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl,haloalkenyl, acyl, aroyl, and heteroaroyl;

[0012] B is formula (V):

[0013] wherein D¹, D², J¹, J² and K¹ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, no more than one of D¹,D², J¹, J² and K¹ can be O, no more than one of D¹, D², J¹, J² and K¹can be S, one of D¹, D², J¹, J² and K¹ must be a covalent bond when twoof D¹, D², J¹, J² and K¹ are O and S, and no more than four of D¹, D²,J¹, J² and K¹ can be N with the proviso that R³², R³³, R³⁴, R³⁵, and R₃₆are each independently selected to maintain the tetravalent nature ofcarbon, trivalent nature of nitrogen, the divalent nature of sulfur, andthe divalent nature of oxygen;

[0014] R³², R³³, R³⁴, R³⁵, and R³⁶ can indedpendently be Q^(b); R⁹, R¹⁰,R¹¹, R¹², R¹³, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R³², R³³, R³³, R³⁴, R³⁵, and R³⁶ areindependently selected from the group consisting of hydrido, amidino,guanidino, dialkylsulfonium, trialkylphosphonium, dialkylsulfoniumalkyl,carboxy, heteroaralkylthio, heteroaralkoxy, cycloalkylamino, acylalkyl,acylalkoxy, aryloylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl,aralkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl,aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl,halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl,cycloalkylsulfinylalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl,heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl,haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl,heteroaralkoxy, cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl,cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy,halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxy,halocycloalkenyloxyalkyl, hydroxy, amino, alkoxyamino, thio, nitro,lower alkylamino, alkylthio, alkylthioalkyl, arylamino, aralkylamino,arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl,alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfonylalkyl,heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl,alkylsulfonylalkyl, haloalkylsulfinylalkyl, haloalkylsulfonylalkyl,alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkylamidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl,arylsulfonamido, diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl,arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl,heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl,alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl,haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky,alkylenedioxy, haloalkylenedioxy, cycloalkyl, cycloalkylalkanoyl,cycloalkenyl, lower cycloalkylalkyl, lower cycloalkenylalkyl, halo,haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl,hydroxyalkyl, aminoalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl,aralkyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl,partially saturated heterocyclyl, heteroaryl, heteroaryloxy,heteroaryloxyalkyl, arylalkyl, heteroarylalkyl, arylalkenyl,heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido,alkylamidocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl,carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano,carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, anddiaralkoxyphosphonoalkyl;

[0015] R³² and R³³, R³³ and R³⁴, R³⁴ and R³⁵, and R³⁵ and R³⁶ can beindependently selected to form a spacer pair wherein a spacer pair istaken together to form a linear moiety having from 3 through 6contiguous atoms connecting the points of bonding of said spacer pairmembers to form a ring selected from the group consisting of acycloalkenyl ring having 5 through 8 contiguous members, a partiallysaturated heterocyclyl ring having 5 through 8 contiguous members, aheteroaryl ring having 5 through 6 contiguous members, and an aryl withthe proviso that no more than one of the group consisting of spacerpairs R³² and R³³, R³³ and R³⁴, R³⁴ and R³⁵, and and R³⁶ can be used atthe same time;

[0016] R⁹ and R¹⁰, R¹⁰ and R¹¹, R¹¹ and R¹², and R¹² and R¹³ can beindependently selected to form a spacer pair wherein a spacer pair istaken together to form a linear moiety having from 3 through 6contiguous atoms connecting the points of bonding of said spacer pairmembers to form a ring selected from the group consisting of acycloalkenyl ring having 5 through 8 contiguous members, a partiallysaturated heterocyclyl ring having 5 through 8 contiguous members, aheteroaryl ring having 5 through 6 contiguous members, and an aryl withthe proviso that no more than one of the group consisting of spacerpairs R⁹ and R¹⁹, R¹⁰ and R¹¹, R¹¹ and R¹², and R¹² and R¹³ can be usedat the same time;

[0017] B can be formula (VI):

[0018] wherein D³, D⁴, J³, and J⁴ are independently selected from thegroup consisting of C, N, O, and S, no more than one of D³, D⁴, J³, andJ⁴ can be O, no more than one of D³, D⁴, J³, and J⁴ can be S, and nomore than three of D¹, D², J¹, and J² can be N with the proviso thatR³², R³³, R³⁴, and R³⁵ are each independently selected to maintain thetetravalent nature of carbon, trivalent nature of nitrogen, the divalentnature of sulfur, and the divalent nature of oxygen;

[0019] B can be selected from the group consisting of C3-C8 alkyl, C3-C8alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl whereineach member of group B may be optionally substituted at any carbon up toand including 6 atoms from the point of attachment of B to A with one ormore of the group consisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆;

[0020] B can be selected from the group consisting of C3-C10 cycloalkyl,C5-C₁₀ cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9 partiallysaturated heterocyclyl, wherein each ring carbon may be optionallysubstituted with R₃₃, a ring carbon other than the ring carbon at thepoint of attachment of B to A may be optionally substituted with oxoprovided that no more than one ring carbon is substituted by oxo at thesame time, ring carbon and nitrogen atoms adjacent to the carbon atom atthe point of attachment may be optionally substituted with R₉ or R₁₃, aring carbon or nitrogen atom adjacent to the R₉ position and two atomsfrom the point of attachment may be substituted with R₁₀, a ring carbonor nitrogen atom adjacent to the R₁₃ position and two atoms from thepoint of attachment may be substituted with R₁₂, a ring carbon ornitrogen atom three atoms from the point of attachment and adjacent tothe R₁₀ position may be substituted with R₁₁, a ring carbon or nitrogenatom three atoms from the point of attachment and adjacent to the R₁₂position may be substituted with R₃₃, and a ring carbon or nitrogen atomfour atoms from the point of attachment and adjacent to the R₁₁ and R₃₃positions may be substituted with R₃₄;

[0021] A is selected from the group consisting of single covalent bond,(W⁷)_(rr)—(CH(R¹⁵))_(pa) and (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is aninteger selected from 0 through 1, pa is an integer selected from 0through 6, and W⁷ is selected from the group consisting of O, S, C(O),C(S), C(O)S, C(S)O, C(O)N(R⁷), C(S)N(R⁷), (R⁷)NC(O), (R⁷)NC(S), S(O),S(O)₂, S(O)₂N(R⁷), (R⁷)NS(O)₂, Se(O), Se(O)₂, Se(O)₂N(R⁷), (R⁷)NSe(O)₂,P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), C(NR⁷)N(R⁷), (R⁷)NC(NR⁷), andN(R⁷) with the proviso that no more than one of the group consisting ofrr and pa can be 0 at the same time;

[0022] R⁷ and R⁸ are independently selected from the group consisting ofhydrido, hydroxy, alkyl, alkenyl, aryl, aralkyl, aryloxy, alkoxy,alkenyloxy, alkylthio, alkylamino, arylthio, arylamino, acyl, aroyl,heteroaroyl, aralkoxyalkyl, heteroaralkoxyalkyl, aryloxyalkyl,alkoxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl,aralkoxyalkyl, heteroaralkoxyalkyl, alkylsulfinylalkyl,alkylsulfonylalkyl, heteroaryl, heteroaryloxy, heteroarylamino,heteroaralkyl, heteroaralkyloxy, heteroaralkylamino, andheteroaryloxyalkyl;

[0023] R¹⁴, R¹⁵, R³⁷, R³⁸, R³⁹, R⁴⁰, R⁴¹ and R⁴² are independentlyselected from the group consisting of hydrido, hydroxy, halo, cyano,aryloxy, amino, alkylamino, dialkylamino, hydroxyalkyl, aminoalkyl,acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, sulfhydryl, acylamido,alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, aralkyl,aryloxyalkyl, aralkoxyalkylalkoxy, alkylsulfinylalkyl,alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkoxythioalkyl,alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl,arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl,cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl,halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl,halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl,saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl,heteroarylalkyl, heteroaiylthioalkyl, heteroaralkylthioalkyl,monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl,carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfinyl,haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl,arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl,cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl,heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl,heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl,carboxy, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl,carboaralkoxy, trialkylsilyl, dialkoxyphosphono, diaralkoxyphosphono,dialkoxyphosphonoalkyl, and diaralkoxyphosphonoalkyl with the provisothat R³⁷ and R³⁸ are independently selected from an acyl other thanformyl

[0024] R¹⁴ and R¹⁴, when bonded to different carbons, can be takentogether to form a group selected from the group consisting of covalentbond, alkylene, haloalkylene, and a linear moiety spacer selected toform a ring selected from the group consisting of cycloalkyl ring havingfrom 5 through 8 contiguous members, cycloalkenyl ring having from 5through 8 contiguous members, and a heterocyclyl having from 5 through 8contiguous members;

[0025] R¹⁴ and R¹⁵, when bonded to different carbons, can be takentogether to form a group selected from the group consisting of covalentbond, alkylene, haloalkylene, and a linear moiety spacer selected toform a ring selected from the group consisting of a cycloalkyl ringhaving from 5 through 8 contiguous members, a cycloalkenyl ring havingfrom 5 through 8 contiguous members, and a heterocyclyl having from 5through 8 contiguous members;

[0026] R¹⁵ and R¹⁵, when bonded to different carbons, can be takentogether to form a group selected from the group consisting of covalentbond, alkylene, haloalkylene, and a linear moiety spacer selected toform a ring selected from the group consisting of cycloalkyl ring havingfrom 5 through 8 contiguous members, cvcloalkenyl ring having from 5through 8 contiguous members, and a heterocyclyl having from 5 through 8contiguous members;

[0027] Ψ is selected from the group consisting of NR⁵, O, C(O), C(S), S,S(O), S(O)₂, ON(R⁵), P(O)(R⁸), and CR³⁹R⁴⁰ with the provisos that Ψ isselected from other than NR⁵, O, S, S(O), and S(O)₂ unless any two ofX⁰, R², R¹, and J are other than hydrido, or that Ψ is selected fromother than O, unless A is selected from other than methylene when B isphenyl, that Ψ is selected from other than C(O), unless A is selectedfrom other than methyleneoxy when B is phenyl, or that Ψ is selectedfrom other than NH unless A is selected from other than a singlecovalent bond when B is acyl, or that Ψ is selected from other than NHunless A is selected from other than S(O) or S(O)₂ when B is phenyl;

[0028] R⁵ is selected from the group consisting of hydrido, alkyl,alkenyl, alkynyl, aryl, aralkyl, aryloxy, alkoxy, alkenyloxy, alkylthio,arylthio, aralkoxyalkyl, heteroaralkoxyalkyl, aryloxyalkyl, alkoxyalkyl,alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, aralkoxyalkyl,heteroaralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, cycloalkyl,cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl,haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl,haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxyalkyl,halocycloalkenyloxyalkyl, heteroaryl, heteroarylalkyl,monocarboalkoxyalkyl, monocarboalkoxy, dicarboalkoxyalkyl,monocarboxamido, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl,acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, anddialkoxyphosphonoalkyl;

[0029] R³⁹ and R⁴⁰, when bonded to the same carbon, can be takentogether to form a group selected from a group consisting of oxo,thiono, R⁵—N, alkylene, haloalkylene, and a linear moiety spacer havingfrom 2 through 7 contiguous atoms to form a ring selected from the groupconsisting of a cycloalkyl ring having from 3 through 8 contiguousmembers, a cycloalkenyl ring having from 3 through 8 contiguous members,and a heterocyclyl ring having from 3 through 8 contiguous members;

[0030] X⁰, R² and R¹ are independently selected from the groupconsisting of Z⁰-Q, hydrido, alkyl, alkenyl, and halo;

[0031] X⁰, R² and R¹ can be independently selected from the groupconsisting of amidino, guanidino, dialkylsulfonium, trialkylphosphonium,dialkylsulfoniumalkyl, heteroarylamino, amino, nitro, alkylamino,arylamino, aralkylamino, alkanoyl, alkenoyl, aroyl, heteroaroyl,aralkanoyl, heteroaralkanoyl, haloalkanoyl, hydroxyhaloalkyl, cyano, andphosphono;

[0032] X⁰ and R¹ can be taken together to form a spacer pair wherein thespacer pair forms a linear moiety having from 3 through 6 contiguousatoms connecting the points of bonding of said spacer pair members toform a ring selected from the group consisting of a cycloalkenyl ringhaving from 5 through 8 contiguous members and a partially saturatedheterocyclyl ring having from 5 through 8 contiguous members with theproviso that no more than one of the group consisting of spacer pair X⁰and R¹ and spacer pair R² and R¹ can be used at the same time;

[0033] X⁰ and R⁵ can be taken together to form a spacer pair wherein thespacer pair forms a linear spacer moiety having from 2 through 5contiguous atoms connecting the points of bonding of said spacer pairmembers to form a heterocyclyl ring having from 5 through 8 contiguousmembers;

[0034] X⁰ and R⁵ can be taken together to form a spacer pair wherein thespacer pair forms a linear spacer moiety having from 2 through 5contiguous atoms connecting the points of bonding of said spacer pairmembers to form a heterocyclyl ring having from 5 through 8 contiguousmembers;

[0035] X⁰ and R⁴⁰ can be taken together to form a spacer pair whereinthe spacer pair forms a linear spacer moiety having from 2 through 5contiguous atoms connecting the points of bonding of said spacer pairmembers to form a heterocyclyl ring having from 5 through 8 contiguousmembers;

[0036] X⁰ can be independently selected to form a linear moiety havingfrom 2 through 5 contiguous atoms linked to the points of bonding ofboth R³⁹ and R⁴⁰ to form a heterocyclyl ring having from 5 through 8contiguous members;

[0037] R² and R¹ can be taken together to form a spacer pair wherein thespacer pair forms a linear moiety having from 3 through 6 contiguousatoms connecting the points of bonding of said spacer pair members toform a ring selected from the group consisting of a cycloalkenyl ringhaving from 5 through 8 contiguous members and a partially saturatedheterocyclyl ring having from 5 through 8 contiguous members with theproviso that no more than one of the group consisting of spacer pair X⁰and R¹ and spacer pair R² and R¹ can be used at the same time;

[0038] X⁰ and R¹ and R² and R¹ spacer pairs are selected independentlyto be —W═X—Y═Z— forming a ring selected from the group consisting of aheteroaryl ring having from 5 through 6 contiguous members and an arylwith the proviso that no more than one of the group consisting of spacerpair X⁰ and R¹ and spacer pair R² and R¹ is used at the same time;

[0039] W, X, Y, and Z are independently selected from the groupconsisting of C(R⁹), N, N(R¹⁰), O, S and a covalent bond with theprovisos that one of W, X, Y, and Z is independently selected to be acovalent bond when one of W, X, Y, and Z is selected from the groupconsisting of O and S, no more than one of W, X, Y, and Z is selectedfrom the group consisting of O and S, no more than three of W, X, Y, andZ are selected from the group consisting of N and N(R¹⁰), and C(R⁹), N,N(R¹⁰), O, and S are independently selected to maintain the tetravalentnature of carbon, trivalent nature of nitrogen, the divalent nature ofsulfur, the divalent nature of oxygen, and the aromaticity of the ring;

[0040] R² and R^(4a), R² and R^(4b), R² and R¹⁴, and R² and R¹⁵ can beindependently selected to form spacer pairs wherein a spacer pair istaken together to form a linear moiety having from 2 through 5contiguous atoms connecting the points of bonding of said spacer pairmembers to form a heterocyclyl ring having from 5 through 8 contiguousmembers with the proviso that no more than one of the group of spacerpairs consisting of R² and R^(4a), R² and R^(4b), R² and R¹⁴, and R² andR¹⁵ can be used at the same time;

[0041] R² can be independently selected to form a linear moiety havingfrom 2 through 5 contiguous atoms linked to the points of bonding ofboth R^(4a) and R^(4b) to form a heterocyclyl ring having from 5 through8 contiguous members;

[0042] Z⁰ is selected from the group consisting of covalent single bond,(CR⁴¹R⁴²)_(q) wherein q is an integer selected from 1 through 6,(CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p) wherein g and p are integersindependently selected from O through 3 and W⁰ is selected from thegroup consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,C(O)N(R⁴¹), (R⁴¹)NC(O), C(S)N(R⁴¹), (R⁴¹)NC(S), OC(O)N(R⁴¹),(R⁴¹)NC(O)O, SC(S)N(R⁴¹), (R⁴¹)NC(S)S, SC(O)N(R⁴¹), (R⁴¹)NC(O)S,OC(S)N(R⁴¹), (R⁴¹)NC(S)O, N(R⁴²)C(O)N(R⁴¹), (R⁴¹)NC(O)N(R⁴²),N(R⁴²)C(S)N(R⁴¹), (R⁴¹)NC(S)N(R⁴²), S(O), S(O)₂, S(O)₂N(R⁴¹),N(R⁴¹)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R⁴¹), N(R⁴¹)Se(O)₂, P(O)(R⁸),N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R⁴¹), ON(R⁴¹), and SiR²⁸R²⁹, and(CH(R⁴¹))_(e)—W²—(CH(R⁴²))_(h) wherein e and h are integersindependently selected from 0 through 2 and W² is selected from thegroup consisting of CR⁴¹═CR⁴², CR⁴¹R⁴²═C; vinylidene), and ethynylidene(C≡C; 1,2-ethynyl), with the provisos that R⁴¹ and R⁴² are selected fromother than halo and cyano when directly bonded to N and Z⁰ is directlybonded to the benzene ring, that W⁰ is selected, wherein g is 0, fromother than NHS(O)₂CH₂aryl or N(R⁴¹) unless R⁴¹ is selected from otherthan hydrido, alkyl, or aralkylsulfonyl, and Z⁰ is selected from otherthan OC(O), C(O)N(H), and (H)NC(O), unless Q is selected from other thanphenyl, 2-furyl, 2-thienyl, 4-thiazolyl, 2-pyridyl, 2-naphthyl,1,2-dihydrobenzofuran-5-yl, 1,2-dihydrobenzofuran-6-yl, or1,2benzisoxazol-6-yl, or X⁰ is selected from other than hydrido, halo,or methyl, or R¹ is selected from other than hydrido, fluoro, hydroxy,acetoxy, propanoyloxy, 2-carboxyacetoxy, 2,3 or 4-carboxypropanoyloxy,benzoyloxy, methyl, or methoxy;

[0043] R²⁸ and R²⁹ are independently selected from the group consistingof hydrido, hydroxyalkyl, alkyl, alkenyl, alkynyl, aryl, aralkyl,aryloxyalkyl, acyl, aroyl, aralkanoyl, heteroaroyl, aralkoxyalkyl,alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl,heteroaralkylthioalkyl, alkoxyalkyl, heteroaryloxyalkyl,alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl,cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl,haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl,haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy,halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryl,perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl,heteroarylthioalkyl, heteroaralkylthioalkyl, cyanoalkyl, dicyanoalkyl,carboxamidoalkyl, dicarboxamidoalkyl, cyanocarboalkoxyalkyl,carboalkoxyalkyl, dicarboalkoxyalkyl, cyanocycloalkyl,dicyanocycloalkyl, carboxamidocycloalkyl, dicarboxamidocycloalkyl,carboalkoxycyanocycloalkyl, carboalkoxycycloalkyl,dicarboalkoxycycloalkyl, formylalkyl, acylalkyl, arylsulfinylalkyl,arylsulfonylalkyl, aralkylsulfinyl, cycloalkylsulfinylalkyl,cycloalkylsufonylalkyl, heteroarylsulfonylalkyl,heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl,carboxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyland diaralkoxyphosphonoalkyl;

[0044] R²⁸ and R²⁹ can be taken together to form a linear moiety spacerhaving from 2 through 7 contiguous atoms and forming a ring selectedfrom the group consisting of a cycloalkyl ring having from 3 through 8contiguous members, a cycloalkenyl ring having from 3 through 8contiguous members, and a heterocyclyl ring having from 3 through 8contiguous members;

[0045] Q is formula (II):

[0046] wherein D¹, D², J¹, J² and K¹ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, no more than one of D¹,D², J¹, J² and K¹ can be O, no more than one of D¹, D², J¹, J² and K¹can be S, one of D¹, D², J¹, J² and K¹ must be a covalent bond when twoof D¹, D², J¹, J² and K¹ are O and S, and no more than four of D¹, D²,J¹, J² and K¹ can be N, with the proviso that R⁹, R¹⁰, R¹¹, R¹², and R¹³are each independently selected to maintain the tetravalent nature ofcarbon, trivalent nature of nitrogen, the divalent nature of sulfur, andthe divalent nature of oxygen;

[0047] Q can be formula (III):

[0048] wherein D³, D⁴, J³, and J⁴ are independently selected from thegroup consisting of C, N, O, and S, no more than one of D³, D⁴, J³, andJ⁴ can be O, no more than one of D³, D⁴, J³, and J⁴ can be S, and nomore than three of D¹, D², J¹, and J² can be N with the proviso that R⁹,R¹⁰, R¹¹, and R¹² are each independently selected to maintain thetetravalent nature of carbon, trivalent nature of nitrogen, the divalentnature of sulfur, and the divalent nature of oxygen;

[0049] Q can be selected from the group consisting of alkyl, alkoxy,alkylamino, alkylthio, haloalkylthio, alkenyl, alkynyl, saturatedheterocyclyl, partially saturated heterocyclyl, acyl, aroyl,heteroaroyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl,cycloalkenylalkyl, cycloalkylalkenyl, haloalkyl, haloalkoxy,haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl,haloalkenyloxyalkyl, halocycloalkoxyalkyl, and halocycloalkenyloxyalkylwith the proviso that Q is selected from other than than alkyl oralkenyl unless any one of X⁰, R¹, and J are other than hydrido;

[0050] K is (CR^(4a)R^(4b))_(n) wherein n is an integer selected from 1through 4;

[0051] R^(4a) and R^(4b) are independently selected from the groupconsisting of halo, hydrido, hydroxy, cyano, hydroxyalkyl, alkyl,alkenyl, aryl, aralkyl, aralkoxyalkyl, aryloxyalkyl, alkoxyalkyl,heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, aralkylthioalkyl,arylthioalkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, haloalkenyl,heteroaryl, heteroarylalkyl, heteroarylthioalkyl,heteroaralkylthioalkyl, cyanoalkyl, alkylsulfinylalkyl,alkylsulfonylalkyl, haloalkylsulfinyl, arylsulfinylalkyl,arylsulfonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinylalkyl,aralkylsulfinylalkyl, and aralkylsulfonylalkyl;

[0052] R^(4a) and R^(4b), when bonded to the same carbon, can be takentogether to form a group selected from the group consisting of oxo,thiono, and a linear spacer moiety having from 2 through 7 contiguousatoms connected to form a ring selected from the group consisting of acycloalkyl ring having 3 through 8 contiguous members, a cycloalkenylring having 5 through 8 contiguous members, and a heterocyclyl ringhaving 5 through 8 contiguous members;

[0053] E⁰ is E¹, when K is (CR^(4a)R^(4b))_(n), wherein E¹ is selectedfrom the group consisting of a covalent single bond, O, S, C(O), C(S),C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷), (R⁷)NC(O)S,OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷),(R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, S(O)₂N(R⁷)C(O),C(O)N(R⁷)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R⁷), N(R⁷)Se(O)₂, P(O)(R⁸),N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R⁷), ON(R⁷), SiR²⁸R²⁹, CR^(4a)═CR^(4b),ethynylidene (C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b);

[0054] K can be (CH(R¹⁴))_(j)-T wherein j is selected from a integerfrom 0 through 3 and T is selected from the group consisting of singlecovalent bond, O, S, and N(R⁷) with the proviso that (CH(R¹⁴))_(j) isbonded to the phenyl ring;

[0055] E⁰ is E², when K is (CH(R¹⁴))_(j)-T, wherein E² is selected fromthe group consisting of a covalent single bond, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),(R⁷)NC(O)O, (R⁷)NC(S)S, (R⁷)NC(O)S, (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷),(R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷), (R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷),N(R⁷)S(O)₂, S(O)₂N(H)C(O), C(O)N(H)S(O)₂, Se(O), Se(O)₂, Se(O)₂N(R⁷),N(R⁷)Se(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), and N(R⁷);

[0056] K can be G-(CH(R¹⁵))_(k) wherein k is selected from an integerfrom 1 through 3 and G is selected from the group consisting of O, S,and N(R⁷) with the proviso that R¹⁵ is other than hydroxy, cyano, halo,amino, alkylamino, dialkylamnino, and sulfhydryl when k is 1;

[0057] E⁰ is E³ when K is G-(CH(R¹⁵))_(k) wherein E³ is selected fromthe group consisting of a covalent single bond, O, S, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷), (R⁷)NC(O)S,OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷),(R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, Se, Se(O), Se(O)₂,Se(O)₂N(R⁷), N(R⁷)Se(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R⁷),ON(R⁷), SiR²⁸R²⁹, CR^(4a)═CR^(4b), ethynylidene (C≡C; 1,2-ethynyl), andC═CR^(4a)R^(4b);

[0058] Y⁰ is formula (IV):

[0059] wherein D⁵, D⁶, J⁵, and J⁶ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, K² is independentlyselected from the group consisting of C, and N⁺, no more than one of D⁵,D⁶, J⁵, and J⁶ can be O, no more than one of D⁵, D⁶, J⁵, and J⁶ can beS, one of D⁵, D⁶, J⁵, and J⁶ must be a covalent bond when two of D⁵, D⁶,J⁵, and J⁶ are O and S, no more than three of D⁵, D⁶, J⁵, and J⁶ can beN when K² is N⁺, and no more than four of D⁵, D⁶, J⁵, and J⁶ can be Nwhen K² is carbon with the provisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are eachindependently selected to maintain the tetravalent nature of carbon,trivalent nature of nitrogen, the divalent nature of sulfur, and thedivalent nature of oxygen;

[0060] R¹⁶ and R¹⁷ can be independently taken together to form a linearmoiety spacer having from 3 through 6 contiguous atoms connected to forma ring selected from the group consisting of a cycloalkenyl ring havingfrom 5 through 8 contiguous members, a partially saturated heterocyclylring having from 5 through 8 contiguous members, a heteroaryl havingfrom 5 through 6 contiguous members, and an aryl;

[0061] R¹⁸ and R¹⁹ can be independently taken together to form a linearmoiety spacer having from 3 through 6 contiguous atoms connected to forma ring selected from the group consisting of a cycloalkenyl ring havingfrom 5 through 8 contiguous members, a partially saturated heterocyclylring having from 5 through 8 contiguous members, a heteroaryl havingfrom 5 through 6 contiguous members, and an aryl;

[0062] Q^(b) is selected from the group consisting of NR²⁰R²¹, ³⁰NR²⁰R²¹R²², oxy, alkyl, alkylaminoalkyl, aminoalkyl,dialkylsulfoniumalkyl, and acylamino wherein R²⁰, R²¹, and R²² areindependently selected from the group consisting of hydrido, alkyl,hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkylwith the provisos that no more than one of R²⁰, R²¹, and R²² can behydroxy, alkoxy, alkylamino, amino, and dialkylamino and that R²⁰, R²¹,and R²² must be other than be hydroxy, alkoxy, alkylamino, amino, anddialkylamino when K² is N⁺;

[0063] R²⁰ and R²¹, R²⁰ and R²², and R²¹ and R²² can be independentlyselected to form a spacer pair wherein a spacer pair is taken togetherto form a linear moiety having from 4 through 7 contiguous atomsconnecting the points of bonding of said spacer pair members to form aheterocyclyl ring having 5 through 8 contiguous members with the provisothat no more than one of the group consisting of spacers pairs R²⁰ andR²¹, R²⁰ and R²², and R²¹ and R²² can be used at the same time;

[0064] Q^(b) can be selected from the group consisting ofN(R²⁶)SO₂N(R²³)(R²⁴), N(R²⁶)C(O)OR⁵, N(R²⁶)C(O)SR⁵, N(R²⁶)C(S)OR⁵ andN(R²⁶)C(S)SR⁵ with the proviso that no more than one of R²³, R²⁴, andR²⁶ can be hydroxy, alkoxy, alkylamino, amino, or dialkylamino when twoof the group consisting of R²³, R²⁴, and R²⁶ are bonded to the sameatom;

[0065] Q^(b) can be selected from the group consisting ofdialkylsulfonium, trialkylphosphonium, C(NR²⁵)NR²³R²⁴,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)C(O)N(R²³)(R²⁴), N(R²⁶)C(S)N(R²³)(R²⁴),C(NR²⁵)OR⁵, C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(S)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), CN(R²⁵)SR⁵,C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with the provisos that no more than one ofR²³, R²⁴, and R²⁶ can be hydroxy, alkoxy, alkylamino, amino, ordialkylamino when two of the group consisting of R²³, R²⁴, and R²⁶ arebonded to the same atom and that said Q^(b) group is bonded directly toa carbon atom;

[0066] R²³, R²⁴, R²⁵, and R²⁶ are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino,aminoalkyl, and hydroxyalkyl;

[0067] R²³ and R²⁴ can be taken together to form a linear spacer moietyhaving from 4 through 7 contiguous atoms connecting the points ofbonding to form a heterocyclyl ring having S through 8 contiguousmembers;

[0068] R²³ and R²⁵, R²⁴ and R²⁵, R²⁵ and R²⁶, R²⁴ and R²⁶, and R²³ andR²⁶ can be independently selected to form a spacer pair wherein a spacerpair is taken together from the points of bonding of selected spacerpair members to form the group L—U—V wherein L, U, and V areindependently selected from the group consisting of O, S, C(O), C(S),C(J_(H))₂S(O), SO₂, OP(OR³¹)R³⁰, P(O)R³⁰, P(S)R³⁰, C(R³⁰)R³¹,C═C(R³⁰)R³¹, (O)₂POP(O)₂, R³⁰(O)POP(O)R³⁰, Si(R²⁹)R²⁸,Si(R²⁹)R²⁸Si(R²⁹)R²⁸, Si(R²⁹)R²⁸OSi(R²⁹)R²⁸, (R²⁸)R²⁹COC(R²⁸)R²⁹,(R²⁸)R²⁹CSC(R²⁸)R²⁹, C(O)C(R³⁰)═C(R³¹), C(S)C(R³⁰)═C(R³¹),S(O)C(R³⁰)═C(R³¹), SO₂C(R³⁰)═C(R³¹, PR³⁰C(R³⁰)═C(R³¹),P(O)R³⁰C(R³⁰)═C(R³¹), P(S)R³⁰C(R³⁰)═C(R³¹), DC(R³⁰)(R³¹)D, OP(OR³¹)R³⁰,P(O)R³⁰, P(S)R³⁰, Si(R²⁸)R²⁹ and N(R³⁰), and a covalent bond with theproviso that no more than any two of L, U and V are simultaneouslycovalent bonds and the heterocyclyl comprised of by L, U, and V has from5 through 10 contiguous member;

[0069] D is selected from the group consisting of oxygen, C═O, C═S,S(O)_(m) wherein m is an integer selected from 0 through 2;

[0070] J_(H) is independently selected from the group consisting ofOR²⁷, SR²⁷ and N(R²⁰)R²¹;

[0071] R²⁷ is selected from the group consisting of hydrido, alkyl,alkenyl, alkynyl, aralkyl, aryloxyalkyl, aralkoxyalkyl,alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl,heteroaralkylthioalkyl, alkoxyalkyl, heteroaryloxyalkyl,alkenyloxyalkyl, alkyfthioalkyl, arylthioalkyl, cycloalkyl,cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl,haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl,haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxyalkyl,halocycloalkenyloxyalkyl, perhaloaryloxyalkyl, heteroaryl,heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl,arylsulfinylalkyl, arylsulfonylalkyl, cycloalkylsulfinylalkyl,cycloalkylsufonylalkyl, heteroarylsulfonylalkyl,heteroarylsulfinylalkyl, aralkylsulfinylalkyl and aralkylsulfonylalkyl;

[0072] R³⁰ and R³¹ are independently selected from hydrido, hydroxy,thiol, aryloxy, amino, alkylamino, dialkylamino, hydroxyalkyl,heteroaryloxyalkyl, alkoxy, allylthio, arylthio, alkyl, alkenyl,alkynyl, aryl, aralkyl, aryloxyalkyl, aralkoxyalkyl, alkylsulfinylalkyl,alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkoxythioalkyl,alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl,arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl,cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl,haloaralkylsulfinylalkyl, aralkylsulfonylalkyl, cyanoalkyl,dicyanoalkyl, carboxamidoalkyl, dicarboxamidoalkyl,cyanocarboalkoxyalkyl, carboalkoxyalkyl, dicarboalkoxyalkyl,cyanocycloalkyl, dicyanocycloalkyl, carboxamidocycloalkyl,dicarboxamidocycloalkyl, carboalkoxycyanocycloalkyl,carboalkoxycycloalkyl, dicarboalkoxycycloalkyl, formylalkyl, acylalkyl,dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, phosphonoalkyl,dialkoxyphosphonoalkoxy, diaralkoxyphosphonoalkoxy, pbosphonoalkoxy,dialkoxyphosphonoalkylamino, diaralkoxypbosphonoalkylamino,phosphonoalkylamino, dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl,sulfonylalkyl, alkoxysulfonylalkyl, aralkoxysulfonylalkyl,alkoxysulfonylalkoxy, aralkoxysulfonylalkoxy, sulfonylalkoxy,alkoxysulfonylalkylamino, aralkoxysulfonylalkylamino, andsulfonylalkylamino;

[0073] R³⁰ and R³¹ can be taken to form a linear moiety spacer grouphaving from 2 through 7 contiguous atoms to form a ring selected fromthe group consisting of a cycloalkyl ring having from 3 through 8contiguous members, a cycloalkenyl ring having from 3 through 8contiguous members, and a heterocyclyl ring having from 3 through 8contiguous members;

[0074] R²³ and R²⁵, R²⁴ and R²⁵, R²⁵ and R²⁶, R²⁴ and R²⁶, R²³ and R²⁶can be independently selected to form a spacer pair wherein a spacerpair is taken together from the points of bonding of selected spacerpair members to form the group L—U—V wherein L, U, and V areindependently selected from the group of 1,2-disubstituted radicalsconsisting of a cycloalkyl radical, a cycdoalkenyl radical whereincycloalkyl and cycloalkenyl radicals are substituted with one or moregroups selected from R³⁰ and R³¹, an aryl radical, an heteroarylradical, a saturated heterocyclic radical and a partially saturatedheterocyclic radical wherein said 1,2-substitutents are independentlyselected from C═O, C═S, C(R²⁸)R³², S(O), S(O)₂, OP(OR³¹)R³⁰, P(O)R³⁰,P(S)R³⁰ and Si(R²⁸)R²⁹;

[0075] R²³ and R²⁵, R²⁴ and R²⁵, R²⁵ and R²⁶, R²⁴ and R²⁶, and R²³ andR²⁶ can be independently selected to form a spacer pair wherein a spacerpair is taken together from the points of bonding of selected spacerpair members to form the group L—U—V wherein L, U, and V areindependently selected from the group of radicals consisting of1,2-disubstituted alkylene radicals and 1,2-disubstituted alkenyleneradical wherein said 1,2-substitutents are independently selected fromC═O, C═S, C(R²⁸)R²⁹, S(O), S(O)₂, OP(OR³¹)R³⁰, P(O)R³⁰, P(S)R³⁰, andSi(R²⁸)R²⁹ and said alkylene and alkenylene radical are substituted withone or more R³⁰ or R³¹ substituents;

[0076] Q^(s) is selected from the group consisting of a single covalentbond, (CR³⁷R³⁸)_(b)—(W⁰)_(az) wherein az is an integer selected frnm 0through 1, b is an integer selected from 1 through 4, and W⁰ is selectedfrom the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S,C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴),SC(S)N(R¹⁴), SC(O)N(R¹⁴), OC(S)N(R¹⁴), N(R¹⁵)C(O)N(R¹⁴),(R¹⁴)NC(O)N(R¹⁵), NR¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵), S(O), S(O)₂,S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R¹⁷), N(R¹⁴)Se(O)₂,P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴), and SiR²⁸R²⁹,(CH(R¹⁴))_(c)—W¹—(CH(R¹⁵)_(d) wherein c and d are integers independentlyselected from 1 through 4, and W¹ is selected from the group consistingof O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(C),C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴), (R¹⁴)NC(O)O, SC(S)N(R¹⁴),(R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S, OC(S)N(R¹⁴), (R¹⁴)NC(S)O,N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵),S(O), S(O)₂, S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R¹⁴),N(R¹⁴)Se(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴),SiR²⁸R²⁹, and (CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) wherein e and h areintegers independently selected from 0 through 2 and W² is selected fromthe group consisting of CR^(4a)═CR^(4b), ethynylidene (C≡C;1,2-ethynyl), and C═CR^(4a)R^(4b) with the provisos that R¹⁴ and R¹⁵ areselected from other than halo and cyano when directly bonded to N andthat (CR³⁷R³⁸)_(b), (CH(R¹⁴))_(c), (CH(R¹⁴))_(e) and are bonded to E⁰;

[0077] R³⁷ and R³⁷, when bonded to different carbons, can be takentogether to form a linear moiety spacer having from 1 through 7contiguous atoms to form a ring selected from the group consisting of acycloalkyl ring having from 3 through 8 contiguous members, acycloalkenyl ring having from 3 through 8 contiguous members, and aheterocyclyl ring having from 3 through 8 contiguous members;

[0078] R³⁸ and R³⁸, when bonded to different carbons, can be takentogether to form a linear moiety spacer having from 1 through 7contiguous atoms to form a ring selected from the group consisting of acycloalkyl ring having from 3 through 8 contiguous members, acycloalkenyl ring having from 3 through 8 contiguous members, and aheterocyclyl ring having from 3 through 8 contiguous members;

[0079] R³⁷ and R³⁸, when bonded to different carbons, can be takentogether to form a linear moiety spacer having from 1 through 7contiguous atoms to form a ring selected from the group consisting of acycloalkyl ring having from 3 through 8 contiguous members acycloalkenyl ring having from 3 through 8 contiguous members, and aheterocyclyl ring having from 3 through 8 contiguous members;

[0080] R³⁷ and R³⁸, when bonded to the same carbon, can be takentogether to form a group selected from a group consisting of oxo,thiono, alkylene, haloalkylene, and a linear moiety spacer having from 2through 7 contiguous atoms to form a ring selected from the groupconsisting of a cycloalkyl ring having from 3 through 8 contiguousmembers, a cycloalkenyl ring having from 3 through 8 contiguous members,and a heterocyclyl ring having from 3 through 8 contiguous members;

[0081] Y⁰ can be Q^(b)-Q^(ss) wherein Q^(ss) is selected from the groupconsisting of (CR³⁷R³⁸)_(f) wherein f is an integer selected from 1through 6, (CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 4, and W¹ is selected from thegroup consisting of W¹ is selected from the group consisting of O, S,C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O),C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴), (R¹⁴)NC(O)O, SC(S)N(R¹⁴),(R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S, OC(S)N(R¹⁴), (R¹⁴)NC(S)O,N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵),S(O), S(O)₂, S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R¹⁴),N(R¹⁴)Se(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴),SiR²⁸R²⁹, and (CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) wherein e and h areintegers independently selected from 0 through 2 and W² is selected fromthe group consisting of CR^(4a)═CR^(4b), ethynylidene (C≡C,1,2-ethynyl), and C═CR^(4a)R^(4b) with the provisos that R¹⁴ and R¹⁵ areselected from other than halo and cyano when directly bonded to N andthat (CR³⁷R³⁸)_(f), (CH(R¹⁵))_(c), and (CH(R¹⁵)_(e) are bonded to E⁰;

[0082] Y⁰ can be Q^(b)-Q^(sss) wherein Q^(sss) is (CH(R³⁸))_(r)—W³, r isan integer selected from 1 through 3, and W³ is selected from the groupconsisting of 1,1-cyclopropyl, 1,2-cyclopropyl, 1,1-cyclobutyl,1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl,1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl,2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl,1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl, 2,3-piperazinyl,2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl,1,4-piperipinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,5-piperidinyl,2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl,1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl,2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl,2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl,2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyranone-2,3-yl,2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl,3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl,2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and3,5-tetrahydropyranyl with the proviso that (CH(R³⁸))_(r) is bonded toE⁰ and Q^(b) is bonded to lowest numbered substituent position of eachW³;

[0083] Y⁰ can be Q^(b)-Q^(sssr) wherein Q^(sssr) is (CH(R³⁸))_(r)—W⁴, ris an integer selected from 1 through 3, and W⁴ is selected from thegroup consisting of 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl,1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl,2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl,3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl,2,3-piperazinyl, 2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl,1,3-piperidinyl, 1,4-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl,2,5-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl,3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl,2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl,2H-2,4-pyranyl, 2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl,4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl,4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofiiranyl,2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl,2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl,3,4-tetrahydropyranyl, and 3,5-tetrahydropyranyl with the provisos that(CH(R³⁸))_(r) is bonded to E⁰ and Q^(b) is bonded to highest numbersubstituent position of each W⁴;

[0084] Y⁰ can be Q^(b)-Q^(ssss) wherein Q^(ssss) is (CH(R³⁸))_(r)—W⁵, ris an integer selected from 1 through 3, and W⁵ is selected from thegroup consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl,3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl,3,5-benzofuranyl, 3,6-benzofuranyl, 3.7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyL3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to lowest number substituent position of each W⁵ andthat (CH(R³⁸))_(r) is bonded to E⁰;

[0085] Y⁰ can be Q^(b)-Q^(ssssr) wherein Q^(ssssr) is (CH(R³⁸))_(r)—W⁶,r is an integer selected from 1 through 3, and W⁶ is selected from thegroup consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl,3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyL 3,4-benzofuranyl,3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to highest number substituent position of each W⁶ andthat (CH(R³⁸))_(r) is bonded to E⁰.

[0086] In an embodiment of compounds of Formula I or a pharmaceuticallyacceptable salt thereof,

[0087] J is selected from the group consisting of hydrido, halo,hydroxy, hydroxyalkyl, amino, aminoalkyl, cyano, alkyl, haloalkyl,carboxy, carboxyalkyl, carboalkoxy, amidocarbonyl, acyl, phosphono,sulfo, O—R⁶, NH—R⁶, S—R⁶, S(O)—R⁶, and S(O)₂—R⁶, wherein R⁶ is selectedfrom the group consisting of alkyl, and haloalkyl, haloalkenyl;

[0088] B is formula (V):

[0089] wherein D¹, D², J¹, J² and K¹ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, no more than one of D¹,D^(2, J) ¹, J² and K¹ are can be O, no more than one of D¹, D², J¹, J²and K¹ can be S, one of D¹, D¹, J¹, J² and K¹ must be a covalent bondwhen two of D¹, D², J¹, J² and K¹ are O and S, and no more than four ofD¹, D², J¹, J² and K¹ can be N with the proviso that R³², R³³, R³⁴, R³⁵,and R³⁶ are each independently selected to maintain the tetravalentnature of carbon, trivalent nature of nitrogen, the divalent nature ofsulfur, and the divalent nature of oxygen;

[0090] R³², R³³, R³⁴, R³⁵ and R³⁶ can independently be Q^(b);

[0091] R⁹, R¹⁰, R¹¹, R¹², R¹³, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R³², R³³, R³⁴, R³⁵and R³⁶ are independently selected from the group consisting of hydrido,amidino, guanidino, dialkylsulfonium, trialkylphosphonium,dialkylsulfoniumalkyl, carboxy, heteroaralkylthio, heteroaralkoxy,cycloalkylamino, acylalkyl, acylalkoxy, aryloylalkoxy, heterocyclyloxy,aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl,perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl,aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl,cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl,cycloalkylsulfonylalkyl, heteroarylamino,N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio,alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy,cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy,cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy,halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl,hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio,alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl,heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl,arylsulfinylalkyl arylsulfonylalkyl, heteroarylsulfinylalkyl,heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl,haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido,alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkylamidosulfonyl, monoarylamidosulfonyl, arylsulfonamido,diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl, arylsulfinyl,arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl,heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl,heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl,alkynyl, alkenyloxy, alkenyloxyalky, alkylenedioxy, haloalkylenedioxy,cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower cycloalkylalkyl,lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, aminoalkyl,hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, aralkyl, aryloxy, aralkoxy,aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl,heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkyl,heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl,carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido,arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl,carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy,phosphono, phosphonoalkyl, diaralkoxyphosphono, anddiaralkoxyphosphonoalkyl;

[0092] R³² and R³³, R³³ and R³⁴, R³⁴ and R³⁵ and R³⁵ and R³⁶ can beindependently selected to form a spacer pair wherein a spacer pair istaken together to form a linear moiety having from 3 through 6contiguous atoms connecting the points of bonding of said spacer pairmembers to form a ring selected from the group consisting of acycloalkenyl ring having 5 through 8 contiguous members, a partiallysaturated heterocyclyl ring having 5 through 8 contiguous members, aheteroaryl ring having 5 through 6 contiguous members, and an aryl withthe proviso that no more than one of the group consisting of spacerpairs R³² and R³³, R³³ and R³⁴, R³⁴ and R³⁵ and R³⁵ and R³⁶ can be usedat the same time;

[0093] R⁹, and R¹⁰, R¹⁰, and R¹¹, R¹¹, and R¹², and R¹² and R¹³, can beindependently selected to forma spacer pair wherein a spacer pair istaken together to form a linear moiety having from 3 through 6contiguous atoms connecting the points of bonding of said spacer pairmembers to form a ring selected from the group consisting of acycloalkenyl ring having 5 through 8 contiguous members, a partiallysaturated heterocyclyl ring having 5 through 8 contiguous members, aheteroaryl ring having 5 through 6 contiguous members, and an aryl withthe proviso that no more than one of the group consisting of spacerpairs R⁹ and R¹⁰, R¹⁰, and R¹¹, R¹¹ and R¹², and R¹² and R¹³, can beused at the same time;

[0094] B can be selected from the group consisting of C3-C8 alkyl, C3-C8alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl whereineach member of group B may be optionally substituted at any carbon up toand including 6 atoms from the point of attachment of B to A with one ormore of the group consisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆;

[0095] B can be selected from the group consisting of C3-C10 cycloalkyl,C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9 partiallysaturated heterocyclyl, wherein each ring carbon may be optionallysubstituted with R₃₃, a ring carbon other than the ring carbon at thepoint of attachment of B to A may be optionally substituted with oxoprovided that no more than one ring carbon is substituted by oxo at thesame time, ring carbon and nitrogen atoms adjacent to the carbon atom atthe point of attachment may be optionally substituted with R₉ or R₁₃, aring carbon or nitrogen atom adjacent to the R₉ position and two atomsfrom the point of attachment may be substituted with R₁₀, a ring carbonor nitrogen atom adjacent to the R₁₃ position and two atoms from thepoint of attachment may be substituted with R₁₂, a ring carbon ornitrogen atom three atoms from the point of attachment and adjacent tothe R₁₀ position may be substituted with R₁₁, a ring carbon or nitrogenatom three atoms from the point of attachment and adjacent to the R₁₂position may be substituted with R₃₃, and a ring carbon or nitrogen atomfour atoms from the point of attachment and adjacent to the R₁₁ and R₃₃positions may be substituted with R₃₄;

[0096] A is selected from the group consisting of single covalent bond,(W⁷)_(rr)—(CH(R¹⁵))_(pa) and (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is aninteger selected from 0 through 1, pa is an integer selected from 0through 6, and W⁷ is selected from the group consisting of O, S, C(O),C(S), C(O)S, C(S)O, C(O)N(R⁷), C(S)N(R⁷), (R⁷)NC(O), (R⁷)NC(S), S(O),S(O)₂, S(O)₂N(R⁷), (R⁷)NS(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷),C(NR⁷)N(R⁷), (R⁷)NC(NR⁷), and N(R⁷) with the proviso that no more thanone of the group consisting of rr and pa can be 0 at the same time;

[0097] R⁷, and R⁸ are independently selected from the group consistingof hydrido, hydroxy, alkyl, acyl, aroyl, heteroaroyl, and alkoxyalkyl;

[0098] R¹⁴, R¹⁵, R³⁷, and R³⁸ are independently selected from the groupconsisting of hydrido, hydroxy, halo, cyano, hydroxyalkyl, alkoxy,alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl,cycloalkenylalkyl, haloalkyl, haloalkenyl, haloalkoxy, haloalkoxyalkyl,haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl,halocycloalkenyloxyalkyl, carboxy, carboxyalkyl, carboalkoxy,carboxamide, and carboxamidoalkyl;

[0099] Ψ is selected from the group consisting of NR, O, C(O), C(S), S,S(O), S(O)₂, ON(R⁵), P(O)(R⁸), and CR³⁹R⁴⁰ with the provisos that Ψ isselected from other than NR⁵, O, S, S, (O), and S(O)₂ unless any two ofX⁰, R², R¹, and J are other than hydrido, or that Ψ is selected fromother than O, unless A is selected from other than methylene when B isphenyl, that Ψ is selected from other than C(O), unless A is selectedfrom other than methyleneoxy when B is phenyl, or that Ψ is selectedfrom other than NH unless A is selected from other than a singlecovalent bond when B is acyl, or that Ψ is selected from other than NHunless A is selected from other than S(O) or S(O)₂ when B is phenyl;

[0100] R⁵ is selected from the group consisting of hydrido, alkyl,alkoxy, alkoxyalkyl, haloalkyl, acyl, aroyl, and heteroaroyl;

[0101] R³⁹, and R⁴⁰ are independently selected from the group consistingof hydrido, hydroxy, halo, cyano, hydroxyalkyl, acyl, aroyl,heteroaroyl, acylamido, alkoxy, alkyl, alkoxyalkyl, haloalkyl,haloalkoxy, haloalkoxyalkyl, alkylsulfonyl, haloalkylsulfonyl, carboxy,carboxyalkyl, carboalkoxy, carboxamide, and carboxamidoalkyl;

[0102] X⁰, R² and R¹ are independently selected from the groupconsisting of Z⁰-Q, hydrido, alkyl, alkenyl, and halo;

[0103] X⁰, R² and R¹ can be independently selected from the groupconsisting of amidino, guanidino, dialkylsulfonium, trialkylphosphonium,dialkylsulfoniumalkyl, heteroarylamino, amino, nitro, alkylamino,arylamino, aralkylamino, alkanoyl, alkenoyl, aroyl, heteroaroyl,aralkanoyl, heteroaralkanoyl, haloalkanoyl, hydroxyhaloalkyl, cyano, andphosphono;

[0104] X⁰ and R¹ can be taken together to form a spacer pair wherein thespacer pair forms a linear moiety having from 3 through 6 contiguousatoms connecting the points of bonding of said spacer pair members toform a ring selected from the group consisting of a cycloalkenyl ringhaving from 5 through 8 contiguous members and a partially saturatedheterocyclyl ring having from 5 through 8 contiguous members with theproviso that no more than one of the group consisting of spacer pair X⁰and R¹ and spacer pair R² and R¹ can be used at the same time;

[0105] R² and R¹ can be taken together to form a spacer pair wherein thespacer pair forms a linear moiety having from 3 through 6 contiguousatoms connecting the points of bonding of said spacer pair members toform a ring selected from the group consisting of a cycloalkenyl ringhaving from 5 through 8 contiguous members and a partially saturatedheterocyclyl ring having from 5 through 8 contiguous members with theproviso that no more than one of the group consisting of spacer pair X⁰and R¹ and spacer pair R² and R¹ can be used at the same time;

[0106] X⁰ and R¹ and R² and R¹ spacer pairs are selected independentlyto be —W═X—Y═Z— forming a ring selected from the group consisting of aheteroaryl ring having from 5 through 6 contiguous members and an arylwith the proviso that no more than one of the group consisting of spacerpair X⁰ and R¹ and spacer pair R² and R¹ is used at the same time;

[0107] W, X, Y, and Z are independently selected from the groupconsisting of C(R⁹), N, N(R¹⁰), O, S and a covalent bond with theprovisos that one of W, X, Y, and Z is independently selected to be acovalent bond when one of W, X, Y, and Z is selected from the groupconsisting of O and S, no more than one of W, X, Y, and Z is selectedfrom the group consisting of O and S, no more than three of W, X, Y, andZ are selected from the group consisting of N and N(R¹⁰), and C(R⁹), N,N(R¹⁰), O, and S are independently selected to maintain the tetravalentnature of carbon, trivalent nature of nitrogen, the divalent nature ofsulfur, the divalent nature of oxygen, and the aromaticity of the ring;

[0108] Z⁰ is selected from the group consisting of covalent single bond,(CR⁴¹R⁴²)_(q) wherein q is an integer selected from 1 through 6,(CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p) wherein g and p are integersindependently selected from 0 through 3 and W⁰ is selected from thegroup consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,C(O)N(R⁴¹), (R⁴¹)NC(O), C(S)N(R⁴¹), (R⁴¹)NC(S), OC(O)N(R⁴¹),(R⁴¹)NC(O)O, SC(S)N(R⁴¹), (R⁴¹)NC(S)S, SC(O)N(R⁴¹), (R⁴¹)NC(O)S,OC(S)N(R⁴¹), (R⁴¹)NC(S)O, N(R⁴²)C(O)N(R⁴¹), (R⁴¹)NC(O)N(R⁴²),N(R⁴²)C(S)N(R⁴¹), (R⁴¹)NC(S)N(R⁴²), S(O), S(O)₂, S(O)₂N(R⁴¹),N(R⁴¹)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R⁴¹), ON(R⁴¹),and (CH(R⁴¹))_(e)—W²—(CH(R⁴²))_(h) wherein e and h are integersindependently selected from 0 through 2 and W² is selected from thegroup consisting of CR⁴¹═CR⁴², CR⁴¹R⁴²═C; vinylidene), and ethynylidene(C≡C; 1,2-ethynyl), with the provisos that R⁴¹ and R⁴² are selected fromother than halo and cyano when directly bonded to N and Z⁰ is directlybonded to the benzene ring, that W⁰ is selected, wherein g is 0, fromother than NHS(O)₂CH₂aryl or N(R⁴¹) unless R⁴¹ is selected from otherthan hydrido, alkyl, or aralkylsulfonyl, and Z⁰ is selected from otherthan OC(O), C(O)N(H), and (H)NC(O), unless Q is selected from other thanphenyl, 2-furyl, 2-thienyl, 4-thiazolyl, 2-pyridyl, 2-naphthyl,1,2-dihydrobenzofuran-5-yl, 1,2-dihydrobenzofuranyl, or1,2-benzisoxazol-yl , or X⁰ is selected from other than hydrido, halo,or methyl, or R¹ is selected from other than hydrido, fluoro, hydroxy,acetoxy, propanoyloxy, 2-carboxyacetoxy, 2,3 or 4-carboxypropanoyloxy,benzoyloxy, methyl, or methoxy;

[0109] R⁴¹, and R⁴² are independently selected from the group consistingof hydrido, hydroxy, halo, cyano, aryloxy, hydroxyalkyl, acyl, aroyl,heteroaroyl, heteroaryloxyalkyl, alkoxy, alkyl, aryl, aralkyl,aryloxyalkyl, aralkoxyalkylalkoxy, alkoxyalkyl, heteroaryloxyalkyl,cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl,cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl,halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl,halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl,saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl,heteroaralkyl, heteroarylthioalkyl, heteroaralkylthioalkyl,alkylsulfonyl, haloalkylsulfonyl, arylsulfonyl, arylsulfonylalkyl,aralkylsulfonyl, cycloalkylsulfonyl, cycloalkylsufonylalkyl,heteroarylsulfonylalkyl, heteroarylsulfonyl, and aralkylsulfonylalkyl;

[0110] Q is formula (II):

[0111] wherein D¹, D², J¹, J² and K¹ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, no more than one of D¹,D², J¹, J³ and K¹ can be O, no more than one of D¹, D², J¹, J² and K¹can be S, one of D¹, D², J¹, J² and K¹ must be a covalent bond when twoof D¹, D², J¹, J² and K¹ are O and S, and no more than four of D¹, D²,J¹, J² and K¹ can be N, with the proviso that R⁹, R¹⁰, R¹¹, R¹², and R¹³are each independently selected to maintain the tetravalent nature ofcarbon, trivalent nature of nitrogen, the divalent nature of sulfur, andthe divalent nature of oxygen;

[0112] Q can be formula (III):

[0113] wherein D¹, D¹, J¹, and J² are independently selected from thegroup consisting of C, N, O, and S, no more than one of D³, D⁴, J³, andJ⁴ can be O, no more than one of D³, D¹, J³ and J⁴ can be S, and no morethan threeof D¹, D², J¹, and J² can be N with the proviso that R⁹, R¹⁰,R¹¹, and R¹² are each independently selected to maintain the tetravalentnature of carbon, trivalent nature of nitrogen, the divalent nature ofsulfur, and the divalent nature of oxygen;

[0114] Q can be selected from the group consisting of alkyl, alkoxy,alkyl amino, alkylthio, haloalkylthio, alkenyl, alkynyl, saturatedheterocyclyl, partially saturated heterocyclyl, acyl, aroyl,heteroaroyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl,cycloalkenylalkyl, cycloalkylalkenyl, haloalkyl, haloalkoxy,haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl,haloalkenyloxyalkyl, halocycloalkoxyalkyl, and halocycloalkenyloxyalkylwith the proviso that Q is selected from other than than alkyl oralkenyl unless any one of X⁰, R¹, and J are other than hydrido;

[0115] K is (CR^(4a)R^(4b))_(n) wherein n is an integer selected from 1through 2;

[0116] R^(4a), and R^(4b) are independently selected from the groupconsisting of halo, hydrido, hydroxy, cyano, hydroxyalkyl, alkyl,alkenyl, alkoxyalkyl, haloalkyl, haloalkenyl, and cyanoalkyl;

[0117] R^(4a) and R^(4b), when bonded to the same carbon, can be takentogether to form a group selected from the group consisting of oxo, anda linear spacer moiety having from 2 through 7 contiguous atomsconnected to form a ring selected from the group consisting of acycloalkyl ring having 3 through 8 contiguous members, a cycloalkenylring having 5 through 8 contiguous members, and a heterocyclyl ringhaving 5 through 8 contiguous members;

[0118] E⁰ is E¹, when K is (CR^(4a)R^(4b))_(n), wherein E¹ is selectedfrom the group consisting of a covalent single bond, O, S, C(O), C(S),C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷), (R⁷)NC(O)S,OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷),(R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, S(O)₂N(R⁷)C(O),C(O)N(R⁷)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)N(R⁸), N(R⁷), ON(R⁷),CR^(4a)═CR^(4b), ethynylidene (C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b);

[0119] K can be (CH(R¹⁴))_(j)-T wherein j is selected from a integerfrom 0 through 2 and T is selected from the group consisting of singlecovalent bond, O, S, and N(R⁷) with the proviso that (CH(R¹⁴))_(j) isbonded to the phenyl ring;

[0120] E⁰ is E², when K is (CH(R¹⁴)_(j)-T, wherein E² is selected fromthe group consisting of a covalent single bond, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),(R⁷)NC(O)O, (R⁷)NC(S)S, (R⁷)NC(O)S, (R⁷)NC(S)O, N(R⁷)C(O)N(R⁷),(R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷), (R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷),N(R⁷)S(O)₂, S(O)₂N(H)C(O), C(O)N(H)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸),P(O)(R⁸)N(R⁷), and N(R⁷);

[0121] K can be G-(CH(R¹⁵))_(k) wherein k is selected from an integerfrom 1 through 2 and G is selected from the group consisting of O, S,and N(R⁷) with the proviso that R¹⁵ is other than hydroxy, cyano, halo,amino, alkylamino, dialkylamino, and sulfhydryl when k is 1;

[0122] E⁰ is E³ when K is G-(CH(R¹⁵))_(k) wherein E³ is selected fromthe group consisting of a covalent single bond, O, S, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷), (R⁷)NC(O)S,OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷),(R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, P(O)(R⁸),N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R⁷), ON(R⁷), CR^(4a)═CR^(4b),ethynylidene (C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b);

[0123] Y⁰ is formula (IV):

[0124] wherein D⁵, D⁶, J⁵, and J⁶ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, K² is independentlyselected from the group consisting of C, and N⁺, no more than one of D⁵,D⁶, J⁵, and J⁶ can be O, no more than one of D⁵, D⁶, J⁵, and J⁶ can beS, one of D⁵, D⁶, J⁵, and J⁶ must be a covalent bond when two of D⁵, D⁶,J⁵, and J⁶ are O and S, no more than three of D⁵, D⁶, J⁵, and J⁶ can beN when K² is N⁺, and no more than four of D⁵, D⁶, J⁵, and J⁶ can be Nwhen K² is carbon with the provisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are eachindependently selected to maintain the tetravalent nature of carbon,trivalent nature of nitrogen, the divalent nature of sulfur, and thedivalent nature of oxygen;

[0125] R¹⁶, and R¹⁷, can be independently taken together to form alinear moiety spacer having from 3 through 6 contiguous atoms connectedto form a ring selected from the group consisting of a cycloalkenyl ringhaving from 5 through 8 contiguous memnbers, a partially saturatedheterocyclyl ring having from 5 through 8 contiguous members, aheteroaryl having from 5 through 6 contiguous members, and an aryl;

[0126] Q^(b) is selected from the group consisting of NR²⁰R²¹,⁺NR²⁰R²¹R²², oxy, alkyl alkylaminoalkyl, aminoalkyl,dialkylsulfoniumalkyl, and acylamino wherein R²⁰, R²¹, and R²² areindependently selected from the group consisting of hydrido, alkyl,hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkylwith the provisos that no more than one of R²⁰, R²¹, and R²², can behydroxy, alkoxy, alkylamino, amino, and dialkylamino and that R²⁰, R²¹,and R²² must be other than be hydroxy, alkoxy, alkylamino, amino, anddialkylamino when K² is N⁺;

[0127] R²⁰, and R²¹, R²⁰ and R²², and R²¹, and R²², can be independentlyselected to form a spacer pair wherein a spacer pair is taken togetherto form a linear moiety having from 4 through 7 contiguous atomsconnecting the points of bonding of said spacer pair members to formn aheterocyclyl ring having 5 through 8 contiguous members with the provisothat no more than one of the group consisting of spacer pairs R²⁰, andR²¹, R²⁰, and R²², and R²¹, and R²² can be used at the same time;

[0128] Q^(b) can be selected from the group consisting ofN(R²⁶)SO₂N(R²³)(R²⁴), N(R²⁶)C(O)OR⁵, N(R²⁶)C(O)SR⁵, N(R²⁶)C(S)OR⁵ andN(R²⁶)C(S)SR⁵ with the proviso that no more than one of R²³, R²⁴, andR²⁶, can be hydroxy, alkoxy, alkylamino, amino, or dialkylamino when twoof the group consisting of R²³, R²⁴, and R²⁶ are bonded to the sameatom;

[0129] Q^(b) can be selected from the group consisfing ofdialkylsulfrilum, trialkylphosphonium, C(NR²⁵)NR²³R²⁴,N(R²⁶C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)C(O)N(R²³)(R²⁴), N(R²⁶)C(S)N(R²³(R²⁴),C(NR²⁵)OR⁵, C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(S)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(NR²⁵)SR⁵,C(O)NR²³R²⁴ and C(O)NR²³R²⁴ with the provisos that no more than one ofR²³, R²⁴, and R²⁶ can be hydroxy, alkoxy, alkylamino, amino, ordialkylamino when two of the group consisting of R²³, R²⁴, and R²⁶ arebonded to the same atom and that said Q^(b) group is bonded directly toa carbon atom;

[0130] R²³, R²⁴, R²⁵, and R²⁶ are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino,aminoalkyl, and hydroxyalkyl;

[0131] R²³ and R²⁴ can be taken together to form a linear spacer moietyhaving from 4 through 7 contiguous atoms connecting the points ofbonding to form a heterocyclyl ring having 5 through 8 contiguousmembers;

[0132] Q^(s) is selected from the group consisting of a single covalentbond, (CR³⁷R³⁸)_(b)—(W⁰)_(az) wherein az is an integer selected from 0through 1, b is an integer selected from 1 through 4, and W⁰ is selectedfrom the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S,C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O)), C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴),SC(S)N(R¹⁴), SC(O)N(R¹⁴), OC(S)N(R¹⁴), N(R¹⁵)C(O)N(R¹⁴),(R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵), S(O), S(O)₂,S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷),N(R¹⁴), ON(R⁷), (CH(R¹⁴))_(c)—W¹—(CH(R⁷))_(d) wherein c and d areintegers independently selected from 1 through 4, and W¹ is selectedfrom the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S,C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴),(R¹⁴)NC(O)O, SC(S)N(R¹⁴), (R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S,OC(S)N(R¹⁴), (R¹⁴)NC(S)O, N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵),N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵), S(O), S(O)₂, S(O)₂N(R¹⁴),N(R¹⁴)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴),and (CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) wherein e and h are integersindependently selected from 0 through 2 and W² is selected from thegroup consisting of CR^(4a)═CR^(4b), ethynylidene (C≡C; 1,2-ethynyl),and C═CR^(4a)R^(4b) with the provisos that R¹⁴ and R¹⁵ are selected fromother than halo and cyano when directly bonded to N and that(CR³⁷R³⁸)_(b), (CH(R¹⁴))_(c), (CH(R¹⁴))_(e) and are bonded to E⁰;

[0133] Y⁰ can be Q^(b)-Q^(ss) wherein Q^(ss) is selected from the groupconsisting of (CR³⁷R³⁸)_(f) wherein f is an integer selected from 1through 6, (CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 4, and W¹ is selected from thegroup consisting of W¹ is selected from the group consisting of O, S,C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴) (R¹⁴)NC(O),C(S)N(R¹⁴), (R¹⁴)NC(S), OC()N(R¹⁴), (R¹⁴)NC(O)O, SC(S)N(R¹⁴),(R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S, OC(S)N(R¹⁴), (R¹⁴)NC(S)O,N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵),S(O), S(O)₂, S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸),P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴), and (CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h)wherein e and h are integers independently selected from 0 through 2 andW² is selected from the group consisting of CR^(4a)═CR^(4b),ethynylidene (C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b) with the provisosthat R¹⁴ and R¹⁵ are selected from other than halo and cyano whendirectly bonded to N and that (CR³⁷R³⁸)_(f), (CH(R¹⁵))_(c), and(CH(R¹⁵))_(e) are bonded to E⁰;

[0134] Y⁰ can be Q^(b)-Q^(sss) wherein Q^(sss) is (CH(R³⁸))_(r)—W³, r isan integer selected from 1 through 3, and W³ is selected from the groupconsisting of 1,1-cyclopropyl, 1,2-cyclopropyl, 1,1-cyclobutyl,1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl,1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl,2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl,1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperzinyl, 2,3-piperazinyl,2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl,1,4-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,5-piperidinyl,2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl,1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl,2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl,2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl,2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl,2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl,3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl,2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and3,5-tetrahydropyrariyl with the proviso that (CH(R³⁸))_(r) is bonded toE⁰ and Q^(b) is bonded to lowest numbered substituent position of eachW³;

[0135] Y⁰ can be Q^(b)-Q^(sssr) wherein Q^(sssr) is (CH(R³⁸))_(r)—W⁴, ris an integer selected from 1 through 3, and W⁴ is selected from thegroup consisting of 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl,1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl,2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl,3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl,2,3-piperazinyl, 2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl,1,3-piperidinyl, 1,4-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl,2,5-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl,3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl,2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl,2H-2,4-pyranyl, 2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl,4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl,4H-pyranone-2,3-yl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl,2,5-tetrahydrofuranyl, 3,4-tetrahy,drofuranyl, 2,3-tetrahydropyrinyl,2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl,3,4-tetrahydropyranyl, and 3,5-tetrahyd opyranyl with the provisos that(CH(R³⁸))_(f) is bonded to E⁰ and Q^(b) is bonded to highest numbersubstituent position of each W⁴;

[0136] Y⁰ can be Q^(b)-Q^(ssss) wherein Q^(ssss) is (CH(R³⁸))_(r)—W⁵, ris an integer selected from 1 through 3, and W⁵ is selected from thegroup consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,7-indenyl, 2,4-indenyl, 3,4-indenyl,3,7-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl,3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to lowest number substituent position of each W⁵ andthat (CH(R³⁸))_(r) is bonded to E⁰;

[0137] Y⁰ can be Q^(b)-Q^(ssssr) wherein Q^(ssssr) is (CH(R³⁸))_(r)—W⁶,r is an integer selected from 1 through 3, and W⁶ is selected from thegroup consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl,3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl,3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to highest number substituent position of each W⁶ andthat (CH(R³⁸))_(r) is bonded to E⁰.

[0138] In another embodiment of compounds of Formula I or apharmaceutically acceptable salt thereof,

[0139] J is selected from the group consisting of hydrido, halo,hydroxy, hydroxyalkyl, amino, aminoalkyl, cyano, haloalkyl, carboxy,carboxyalkyl, amidocarbonyl, acyl, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ isselected from the group consisting of alkyl and haloalkyl;

[0140] B is formula (V):

[0141] wherein D¹, D², J¹, J² and K¹ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, no more than one of D¹,D², J¹, J² and K¹ can be O, no more than one of D¹, D², J¹, J² and K¹can be S, one of D¹, D², J¹, J² and K¹ must be a covalent bond when twoof D¹, D², J¹, J² and K¹ are O and S, and no more than four of D¹, D²,J¹, J² and K¹ can be N;

[0142] R³², R³³, R³⁴, R³⁵, and R³⁶ can independently be Q^(b);

[0143] R⁹, R¹⁰, R¹¹, R¹², R¹³, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R³², R³³, R³⁴, R³⁵,and R³⁶ are independently selected from the group consisting of hydrido,amidino, guanidino, dialkylsulfonium, trialkylphosphonium,dialkylsulfoniumalkyl, carboxy, heteroaralkylthio, heteroaralkoxy,cycloalkylamino, acylalkyl, acylalkoxy, aryloylalkoxy, heterocyclyloxy,aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl,perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl,aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl,cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl,cycloalkylsulfonylalkyl, heteroarylamino,N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio,alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy,cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy,cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy,halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl,hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio,alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl,heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl,arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl,heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl,haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido,alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkylamidosulfonyl, monoarylamidosulfonyl, arylsulfonamido,diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl, arylsulfinyl,arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl,heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl,heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl,alkynyl, alkenyloxy, alkenyloxyalky, alkylenedioxy, haloalkylenedioxy,cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower cycloalkylalkyl,lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, aminoalkyl,hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, aralkyl, aryloxy, aralkoxy,aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl,heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkyl,heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl,carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido,arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl,carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy,phosphono, phosphonoalkyl, diaralkoxyphosphono, anddiaralkoxyphosphonoalkyl;

[0144] B can be selected from the group consisting of C3-C8 alkyl, C3-C8alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl whereineach member of group B may be optionally substituted at any carbon up toand including 6 atoms from the point of attachment of B to A with one ormore of the group consisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆;

[0145] B canbe selected from the group consisting of C3-C10 cycloalkyl,C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9 partiallysaturated heterocyclyl, wherein each ring carbon may be optionallysubstituted with R₃₃, a ring carbon other than the ring carbon at thepoint of attachment of B to A may be optionally subsfituted with oxoprovided that no more than one ring carbon is substituted by oxo at thesame time, ring carbon and nitrogen atoms adjacent to the carbon atom atthe point f attachment may be optionally substituted with R₉ or R₁₃, aring carbon or nitrogen atom adjacent to the R₉ position and two atomsfrom the point of attachment may be substituted with R₁₀, a ring carbonor nitrogen atom adjacent to the R₁₃ position and two atoms from thepoint of attachment may be substituted with R₁₂, a ring carbon ornitrogen atom three atoms from the point of attachment and adjacent tothe R₁₀ position may be substituted with R₁₁, a ring carbon or nitrogenatom three atoms from the point of attachment and adjacent to the R₁₂position may be substituted with R₃₃, and a ring carbon or nitrogen atomfour atoms from the point of attachment and adjacent to the R₁₁ and R₃₃positions may be substituted with R₃₄;

[0146] A is selected from the group consisting of single covalent bond,(W⁷)_(rr—(CH(R) ¹⁵))_(pa) and (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is aninteger selected from 0 through 1, pa is an integer selected from 0through 6, and W⁷ is selected from the group consisting of O, S, C(O),C(S), C(O)S, C(S)O, C(O)N(R⁷), C(S)N(R⁷), (R⁷)NC(O), (R⁷)NC(S), S(O),S(O)₂, S(O)₂N(R⁷), (R⁷)NS(O)₂, C(NR⁷)N(R⁷), (R⁷)NC(NR⁷), and N(R⁷) withthe proviso that no more than one of the group consisting of rr and pacan be 0 at the same time;

[0147] R⁷ and R⁸ are independently selected from the group consisting ofhydrido, hydroxy, alkyl, and alkoxyalkyl;

[0148] R¹⁴, R¹⁵, R³⁷, and R³⁸ are independently selected from the groupconsisting of hydrido, hydroxy, halo, alkyl, alkoxyalkyl, haloalkyl,haloalkoxy, and haloalkoxyalkyl;

[0149] Ψ is selected from the group consisting of NR⁵, O, C(O), C(S), S,S(O), S(O)₂, and CR³⁹R⁴⁰ with the provisos that Ψ is selected from otherthan NR⁵, O, S, S(O), and S(O)₂ unless any two of X⁰, R², R¹, and J areother than hydrido, or that Ψ is selected from other than O, unless A isselected from other than methylene when B is phenyl, that Ψ is selectedfrom other than C(O), unless A is selected from other than methyleneoxywhen B is phenyl, or that Ψ is selected from other than NH unless A isselected from other than a single covalent bond when B is acyl, or thatΨ is selected from other than NH unless A is selected from other thanS(O) or S(O)₂ when B is phenyl;

[0150] R⁵ is selected from the group consisting of hydrido, alkyl, andalkoxy;

[0151] R³⁹ and R⁴⁰ are independently selected from the group consistingof hydrido, hydroxy, halo, hydroxyalkyl, alkyl, alkoxyalkyl, haloalkyl,haloalkoxy, and haloalkoxyalkyl;

[0152] X⁰, R² and R¹ are independently selected from the groupconsisting of Z⁰-Q, hydrido, alkyl, alkenyl, and halo;

[0153] X⁰, R² and R¹ can be independently selected from the groupconsisting of amidino, guanidino, dialkylsulfonium, trialkylphosphonium,dialkylsulfoniumalkyl, heteroarylamino, amino, nitro, alkylamino,arylamino, aralkylamino, alkanoyl, alkenoyl, aroyl, heteroaroyl,walkanoyl, heteroaralkanoyl, haloalkanoyl, hydroxyhaloalkyl, cyano, andphosphono; Z⁰ is selected from the group consisting of covalent singlebond, (CR⁴¹R⁴²)_(q) wherein q is an integer selected from 1 through 2,(CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p) wherein g and p are integersindependently selected from 0 through 2 and W⁰ is selected from thegroup consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,C(O)N(R⁴¹), (R⁴¹)NC(O), C(S)N(R⁴¹), (R⁴¹)NC(S), OC(O)N(R⁴¹),(R⁴¹)NC(O)O, SC(S)N(R⁴¹), (R⁴¹)NC(S)S, SC(O)N(R⁴¹), (R⁴¹)NC(O)S,OC(S)N(R⁴¹), (R⁴¹)NC(S)O, N(R⁴²)C(O)N(R⁴¹), (R⁴¹)NC(O)N(R⁴²),N(R⁴²)C(S)N(R⁴¹), (R⁴¹)NC(S)N(R⁴²), S(O), S(O)₂, S(O)₂N(R⁴¹),N(R⁴¹)S(O)₂, N(R⁴¹), ON(R⁴¹), and (CH(R⁴¹))_(e)—W²—(CH(R⁴²))_(h) whereine and h are integers independently selected from 0 through 2 and W² isselected from the group consisting of CR⁴¹═CR⁴², CR⁴¹R⁴²═C; vinylidene),and ethynylidene (C≡C; 1,2-ethynyl), with the provisos that R⁴¹ and R⁴²are selected from other than halo and cyano when directly bonded to Nand Z⁰ is directly bonded to the benzene ring, that W⁰ is selected,wherein g is 0, from other than NHS(O)₂CH₂aryl or N(R⁴¹) unless R⁴¹ isselected from other than hydnido, alkyl, or aralkylsulfonyl, and Z⁰ isselected from other than OC(O), C(O)N(H), and (H)NC(O), unless Q isselected from other than phenyl, 2-furyl, 2-thienyl, 4-thiazolyl,2-pyridyl, 2-naphthyl, 1,2-dihydrobenzofuran-5-yl,1,2-dihydrobenzofuran-6-yl, or 1,2benzisoxazol-6-yl , or X⁰ is selectedfrom other than hydrido, halo, or methyl, or R¹ is selected from otherthan hydrido, fluoro, hydroxy, acetoxy, propanoyloxy, 2-carboxyacetoxy,2,3 or 4-carboxypropanoyloxy, benzoyloxy, methyl, or methoxy;

[0154] R⁴¹ and R⁴² are independently selected from the group consistingof hydrido, hydroxy, halo, cyano, aryloxy, hydroxyalkyl, acyl, aroyl,heteroaroyl, heteroaryloxyalkyl, alkoxy, alkyl, aryl, aralkyl,aryloxyalkyl, aralkoxyalkylalkoxy, alkoxyalkyl, heteroaryloxyalkyl,cycloalkyl, cyclbalkylalkyl, cycloalkylalkenyl, cycloalkenyl,cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl,halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl,halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl,saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl,and heteroaralkyl;

[0155] Q is formula (II):

[0156] wherein D¹, D², J¹, J², and K¹ are independently selected fromthe group consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, no more than one of D¹,D², J¹, J² and K¹ can be O, no more than one of D¹, D², J¹, J² and K¹can be S, one of D¹, D², J², J¹, and K¹ must be a covalent bond when twoof D¹, D², J¹, J² and K¹ are O and S, and no more than four of D¹, D²,J¹, J² and K¹ can be N, with the proviso that R⁹, R¹⁰, R¹¹, R¹², and R¹³are each independently selected to maintain the tetravalent nature ofcarbon, trivalent nature of nitrogen, the divalent nature of sulfur, andthe divalent nature of oxygen;

[0157] Q can be selected from the group consisting of alkyl, alkoxy,alkylamino, alkylthio, haloalkylthio, saturated heterocyclyl, alkyl,partially saturated heterocyclyl, acyl, aroyl, heteroaroyl, cycloalkyl,cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, cycloalkylalkenyl,haloalkyl, haoalkoxy, haloalkenyl, halocycloalkyl, halocycloalkenyl,haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxyalkyl, andhalocycloalkenyloxyalkyl;

[0158] K is (CR^(4a)R^(4b))_(n) wherein n is the integer 1;

[0159] R^(4a) and R^(4b) are independently selected from the groupconsisting of halo, hydrido, hydroxy, hydroxyalkyl, alkyl, alkoxyalkyl,and haloalkyl;

[0160] E⁰ is E¹, when K is (CR^(4a)R^(4b))_(n), wherein E¹ is selectedfrom the group consisting of a covalent single bond, O, S, C(O), C(S),C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷), (R⁷)NC(O)S,OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷),(R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, S(O)₂N(R⁷)C(O),C(O)N(R⁷)S(O)₂, N(R⁷), ON(R⁷), CR^(4a)═CR^(4b), ethynylidene (C≡C;1,2-ethynyl), and C═CR^(4a)R^(4b);

[0161] K can be (CH(R¹⁴))_(j)-T wherein j is selected from a integerfrom 0 through 1 and T is selected from the group consisting of singlecovalent bond, O, S, and N(R⁷) with the proviso that (CH(R¹⁴))_(j) isbonded to the phenyl ring;

[0162] E⁰ is E², when K is (CH(R⁷))_(j)-T, wherein E is selected fromthe group consisting of a covalent single bond, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),(R⁷)NC(O)O, (R⁷)NC(S)S, (R⁷)NC(O)S, (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷),(R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷), (R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷),N(R⁷)S(O)₂, S(O)₂N(H)C(O), C(O)N(H)S(O)₂, and N(R⁷);

[0163] K can be G-(CH(R¹⁵))_(k) wherein k is the integer 1 and G isselected from the group consisting of O, S, and N(R⁷);

[0164] E⁰ is E³ when K is G-(CH(R¹⁵))_(k) wherein E³ is selected fromthe group consisting of a covalent single bond, O, S, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),OC(O)N(R⁷),(R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷), (R⁷)NC(O)S,OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷),(R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, N(R⁷), ON(R⁷),CR^(4a)═CR^(4b), ethynylidene (C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b);

[0165] Y⁰ is formula (IV):

[0166] wherein D⁵, D⁶, J⁵, and J⁶ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, K² is independentlyselected from the group consisting of C, and N⁺, no more than one of D⁵,D⁶, J⁵, and J⁶ can be O, no more than one of D⁵, D⁶, J⁵, and J⁶ can beS, one of D⁵, D⁶, J⁵ and J⁶ must be a covalent bond when two of D⁵, D⁶,J⁵, and J⁶ are O and S, no more than three of D⁵, D⁶, J⁵, and J⁶ can beN when K² is N⁺, and no more than four of D⁵, D⁶, J⁵, and J⁶ can be Nwhen K² is carbon with the provisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are eachindependently selected to maintain the tetravalent nature of carbon,trivalent nature of nitrogen, the divalent nature of sulfur, and thedivalent nature of oxygen;

[0167] Q^(b) is selected from the group consisting of NR²⁰R²¹,⁺NR²⁰R²¹R²² oxy, alkyl, alkylaminoalkyl, aminoalkyl,dialkylsulfoniumalkyl, and acylamino wherein R²⁰, R²¹, and R²² areindependently selected from the group consisting of hydrido, alkyl,hydroxy, alkoxy, alkylamino, dialkyl amino, aminoalkyl, and hydroxyalkylwith the provisos that no more than one of R²⁰, R²¹, and R²², can behydroxy, alkoxy, alkylamino, amino, and dialkylamino and that R²⁰, R²¹,and R²² must be other than be hydroxy, alkoxy, alkylamino, amino, anddialkylamino when K² is N⁺;

[0168] Q^(b) can be selected from the group consisting ofN(R²⁶)SO₂N(R²³)(R²⁴), N(R²⁶)C(O)OR⁵, N(R²⁶)C(O)SR⁵, N(R²⁶)C(S)OR⁵, andN(R²⁶)C(S)SR⁵ with the proviso that no more than one of R²³, R²⁴, andR²⁶ can be hydroxy, alkoxy, alkylamino, amino, or dialkylamino when twoof the group consisting of R²³, R²⁴, and R²⁶ are bonded to the sameatom;

[0169] Q^(b) can be selected from the group consisting ofdialkylsulfomium, trialkylphosphonium, C(NR²⁵)NR²³R²⁴,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)C(O)N(R²³(R²⁴), N(R²⁶)C(S)N(R²³)(R²⁴),C(NR²⁵)OR⁵, C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(S)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(NR²⁵)SR⁵,C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with the provisos that no more than one ofR²³, R²⁴, and R²⁶ can be hydroxy, alkoxy, alkylamino, amino, ordialkylamino when two of the group consisting of R²³, R²⁴, and R²⁶ arebonded to the same atom and that said Q^(b) groupis bonded directly to acarbon atom;

[0170] R²³, R²⁴, R²⁵, and R²⁶ are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino,aminoalkyl, and hydroxyalkyl;

[0171] Q^(s) is selected from the group consisting of a single covalentbond, (CR³⁷R³⁸)_(b)—(W⁰)_(az) wherein az is an integer selected from 0through 1, b is an integer selected from 1 through 2, and W⁰ is selectedfrom the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S,C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴),SC(S)N(R¹⁴), SC(O)N(R¹⁴), OC(S)N(R¹⁴), N(R¹⁵)C(O)N(R¹⁴),(R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵), S(O), S(O)₂,S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, N(R¹⁴), ON(R¹⁴), and(CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 2, and W¹ is selected from thegroup consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴),(R¹⁴)NC(O)O, SC(S)N(R¹⁴), (R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S,OC(S)N(R¹⁴), (R¹⁴)NC(S)O, N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R₁₅),N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵), S(O), S(O)₂, S(O)₂N(R¹⁴),N(R¹⁴)S(O)₂, N(R¹⁴), ON(R¹⁴), and (CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) whereine and h are integers independently selected from 0 through 2 and W² isselected from the group consisting of CR^(4a)═CR^(4b), ethynylidene(C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b) with the provisos that R¹⁴ andR¹⁵ are selected from other than halo and cyano when directly bonded toN and that (CR³⁷R³⁸)_(b), (CH(R¹⁴))_(c), (CH(R¹⁴))_(e) and are bonded toE⁰;

[0172] Y⁰ can be Q^(b)-Q^(ss) wherein Q^(ss) is selected from the groupconsisting of (CR³⁷R³⁸)_(f) wherein f is an integer selected from 1through 4, (CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 2, and W¹ is selected from thegroup consisting of W¹ is selected from the group consisting of O, S,C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O),C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴), (R¹⁴)NC(O)O, SC(S)N(R¹⁴),(R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S, OC(S)N(R¹⁴), (R¹⁴)NC(S)O,N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵),S(O), S(O)₂, S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, N(R¹⁴), ON(R¹⁴), and(CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) wherein e and h are integersindependently selected from 0 through 2 and W² is selected from thegroup consisting of CR^(4a)═R^(4b), ethynylidene (C≡C; 1,2-ethynyl), andC═CR^(4a)R^(4b) with the provisos that R¹⁴ and R¹⁵ are selected fromother than halo when directly bonded to N and that (CR³⁷R³⁸)_(f),(CH(R¹⁵))_(c), and (CH(R¹⁵))_(e) are bonded to E⁰;

[0173] Y⁰ can be Q^(b)-Q^(sss) wherein Q^(sss) is (CH(R³⁸))_(r)—W³, r isan integer selected from 1 through 2, and W³ is selected from the groupconsisting of 1,1-cyclopropyl, 1,2-cyclopropyl, 1,1-cyclobutyl,1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl,1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl,2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl,1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl, 2,3-piperazinyl,2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl,1,4-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,5-piperidinyl,2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl,1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl,2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl,2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H2,4-pyranyl, 4H-2,5-pyranyl,2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyran-44-one-2,3-yl,2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl,3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl,2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and3,5-tetrahydropyranyl with the proviso that (CH(R³⁸))_(r) is bonded toE⁰ and Q_(b) is bonded to lowest numbered substituent position of eachW³;

[0174] Y⁰ can be Q^(b)-Q^(sssr) wherein Q^(sssr) is (CH(R³⁸))_(r)—W⁴, ris an integer selected from 1 through 2, and W⁴ is selected from thegroup consisting of 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl,1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl,2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl,3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl,2,3-piperazinyl, 2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl,1,3-piperidinyl, 1,4-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl,2,5-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl,3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrroilidinyl, 2,3-pyrrolidinyl,2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl,2H-2,4-pyranyl, 2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl,4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl,4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl,2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl,2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl,3,4-tetrahydropyranyl, and 3,5-tetrahydropyranyl with the provisos that(CH(R³⁸))_(r) is bonded to E⁰ and Q^(b) is bonded to highest numbersubstituent position of each W⁴;

[0175] Y⁰ can be Q^(b)-Q^(ssss) wherein Q^(ssss) is (CH(R³⁸))_(r)—W⁵, ris an integer selected from 1 through 2, and W⁵ is selected from thegroup consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl,3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl,3,5-benzofuranyi, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,sbenzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to lowest number substituent position of each W⁵ andthat (CH(R³⁸))_(r) is bonded to E⁰;

[0176] Y⁰ can be Q^(b)-Q^(ssssr) wherein Q^(ssssr) (CH(R³⁸))_(r)—W⁶, ris an integer selected from 1 through 2, and W⁶ is selected from thegroup consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl,3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl,3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl,3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl,2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl,3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl,1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl,2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl,2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl,2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl,3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl,4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl,1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl,3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl,3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl,4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl,3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl,4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl withthe proviso that Q^(b) is bonded to highest number substituent positionof each W⁶ and that (CH(R³⁸))_(r) is bonded to E⁰.

[0177] In a preferred embodiment of compounds of Formula I or apharmaceutically acceptable salt thereof,

[0178] J is selected from the group consisting of hydrido, halo,hydroxy, hydroxyalkyl, amino, aminoalkyl, O—R⁶, NH—R⁶, and S—R⁶, whereinR⁶ is selected from the group consisting of alkyl and haloalkyl;

[0179] B is formula (V):

[0180] wherein D¹, D², J¹, J² and K¹ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with theprovisos thatno more than one can be a covalent bond, no more than one of D¹, D², J¹,J² and K¹ can be O, On more than one of D¹, D², J¹, J² and K¹ can be S,one of D¹, D², J¹, J² and K¹ must be a covalent bond when two of D¹, D²,J¹, J² and K¹ are O and S, and no more than four of D¹, D², J¹, J² andK¹ can be N;

[0181] R⁹, R¹⁰, R¹¹, R¹², R¹³, R³², R³³, R³⁴, R³⁵, and R³⁶ areindependently selected from the group consisting of hydrido, amidino,guanidino, dialkylsulfonium, carboxy, haloalkylthio, alkanoyloxy,alkoxy, alkoxyalkyl, haloalkoxylalkyl, hydroxy, amino, alkoxyamino,thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, alkylsulfinyl,alkylsulfinylalkyl, alkylsulfonyl, alkylsulfonylalkyl,haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido,alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkylamidosulfonyl, alkanoyl, alkenoyl, haloalkanoyl, alkyl, alkenyl,alkenyloxy, alkenyloxyalky, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl, haloalkoxyalkyl,carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido,carboalkoxyalkyl, carboalkoxyalkenyl, carboxamido, carboxamidoalkyl, andcyano;

[0182] R³², R³³, R³⁴, R³⁵, and R³⁶ can independently be Q^(b);

[0183] B can be selected from the group consisting of C3-C8 alkyl, C3-C8alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl whereineach member of group B may be optionally substituted at any carbon up toand including 6 atoms from the point of attachment of B to A with one ormore of the group consisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆;

[0184] B can be selected from the group consisting of C3-C10 cycloalkyl,C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9-partiallysaturated heterocyclyl, wherein each ring carbon may be optionallysubstituted with R₃₃, a ring carbon other than the ring carbon at thepoint of attachment of B to A may be optionally substituted with oxoprovided that no more than one ring carbon is substituted by oxo at thesame time, ring carbon and nitrogen atoms adjacent to the carbon atom atthe point of attachment may be optionally substituted with R₉ or R₁₃, aring carbon or nitrogen atom adjacent to the R₉ position and two atomsfrom the point of attachment may be substituted with R₁₀, a ring carbonor nitrogen atom adjacent to the R₁₃ position and two atoms from thepoint of attachment may be substituted with R₁₂, a ring carbon ornitrogen atom three atoms from the point of attachment and adjacent tothe R₁₀ position may be substituted with R₁₁, a ring carbon or nitrogenatom three atoms from the point of attachment and adjacent to the R₁₂position may be substituted with R₃₃, and a ring carbon or nitrogen atomfour atoms from the point of attachment and adjacent to the R₁₁ and R₃₃positions may be substituted with R₃₄;

[0185] A is selected from the group consisting of single covalent bond,(W⁷)_(rr)—(CH(R¹⁵))_(pa) and (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is aninteger selected from 0 through 1, pa is an integer selected from 0through 6, and W⁷ is selected from the group consisting of O, S, C(O),C(S), C(O)S, C(S)O, C(O)N(R⁷), C(S)N(R⁷), (R⁷)NC(O), (R⁷)NC(S), S(O),S(O)₂, S(O)₂N(R⁷), (R⁷)NS(O)₂, C(NR⁷)N(R⁷), (R⁷)NC(NR⁷), and N(R⁷) withthe proviso that no more than one of the group consisting of rr and pacan be 0 at the same time;

[0186] R⁷ and R⁸ are independently selected from the group consisting ofhydrido, hydroxy, alkyl, and alkoxyalkyl;

[0187] R¹⁵ is selected from the group consisting of hydrido, hydroxy,halo, alkyl, and haloalkyl;

[0188] Ψ is NH with the provisos that Ψ is selected from other than NHunless any two of X⁰, R², R¹, and J are other than hydrido or that Ψ isselected from other than NH unless A is selected from other than asingle covalent bond when B is acyl, or that Ψ is selected from otherthan NH unless A is selected from other than S(O) or S(O)₂ when B isphenyl;

[0189] X⁰ is hydrido;

[0190] R¹ is selected from the group consisting of hydrido, alkyl,alkoxy, alkylamino, alkylthio, haloalkylthio, haloalkyl, haloalkoxy, andhalo;

[0191] R² is selected from the group consisting of Z⁰-Q, hydrido, alkyl,alkenyl, and halo;

[0192] Z⁰ is a covalent single bond;

[0193] Q is formula (II):

[0194] wherein D¹, D², J¹, J² and K¹ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, no more than one of D¹,D², J¹, J² and K¹ can be O, no more than one of D¹, D², J¹, J² and K¹can be S, one of D¹, D² J¹, J² and K¹ must be a covalent bond when twoof D¹, D², J¹, J² and K¹ are O and S, and no more than four of D¹, D²,J¹, J² and K¹ can be N, with the proviso that R⁹, R¹⁰, R¹¹, R¹², and R¹³are each independently selected to maintain the tetravalent nature ofcarbon, trivalent nature of nitrogen, the divalent nature of sulfur, andthe divalent nature of oxygen;

[0195] K is CR^(4a)R^(4b);

[0196] R^(4a) and R^(4b) are independently selected from the groupconsisting of halo, hydrido, hydroxy, alkyl, and haloalkyl;

[0197] E⁰ is E¹, when K¹ is CR^(4a)R^(4b), wherein E¹ is selected fromthe group consisting of a covalent single bond, C(O)N(H), (H)NC(O),C(S)N(H), (H)NC(S), S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), andC(O)N(H)S(O)₂;

[0198] K can be (CH(R¹⁴))_(j)-T wherein j is selected from an integerfrom 0 through 1 and T is selected from the group consisting of singlecovalent bond and N(R⁷) with the proviso that (CH(R¹⁴))_(j) is bonded tothe phenyl ring;

[0199] E⁰ is E², when K is (CH(R¹⁴))_(j)-T, wherein E² is selected fromthe group consisting of C(O)N(H), (H)NC(O), C(S)N(H), (H)NC(S),S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0200] R¹⁴ is selected from the group consisting of hydrido, halo,alkyl, and haloalkyl;

[0201] Y⁰ is formula (IV):

[0202] wherein D⁵, D⁶, J⁵, and J⁶ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, K² is independentlyselected from the group consisting of C, and N⁺, no more than one of D⁵,D⁶, J⁵, and J⁶ can be O, no more than one of D⁵, D⁶, J⁵, and J⁶ can beS, one of D⁵, D⁶, J⁵, and J⁶ must be a covalent bond when two of D⁵, D⁶,J⁵, and J⁶ are O and S, no more than three of D⁵, D⁶, J⁵, and J⁶ can beN when K² is N⁺, and no more than four of D⁵, D⁶, J⁵, and J⁶ can be Nwhen K² is carbon with the provisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are eachindependently selected to maintain the tetravalent nature of carbon,trivalent nature of nitrogen, the divalent nature of sulfur, and thedivalent nature of oxygen;

[0203] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, dialkylsulfonium, carboxy,haloalkylthio, alkoxy, hydroxy, amino, thio, nitro, lower alkylamino,alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, alkenoyl,haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboalkoxy,carboalkoxyalkyl, and cyano;

[0204] Q^(b) is selected from the group consisting of NR²⁰R²¹,⁺NR²⁰R²¹R²², oxy, alkyl, alkylaminoalkyl, aminoalkyl,dialkylsulfoniumalkyl, and acylamino wherein R²⁰, R²¹, and R²² areindependently selected from the group consisting of hydrido, alkyl,hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkylwith the provisos that no more than one of R²⁰, R²¹, and R²² can behydroxy, alkoxy, alkylamino, amino, and dialkylamino and that R²⁰, R²¹,and R²² must be other than be hydroxy, alkoxy, alkylamino, amino, anddialkylamino when K² is N⁺;

[0205] Q^(b) can be N(R²⁶)SO₂N(R²³)(R²⁴) with the proviso that no morethan one of R²³, R²⁴, and R²⁶ can be hydroxy, alkoxy, alkylamino, amino,or dialkylamino when two of the group consisting of R²³, R²⁴, and R²⁶are bonded to the same atom;

[0206] Q^(b) can be selected from the group consisting ofdialkylsulfonium, trialkylphosphonium, C(NR²⁵)NR²³R²⁴,N(R²⁶)C(NR²⁵)N(R²³)(R24), N(R²⁶)C(O)N(R²³)(R²⁴), N(R²⁶)C(S)N(R²³)(R²⁴),C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(S)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴,and C(O)NR²³R²⁴ with the provisos that no more than one of R²³, R²⁴, andR²⁶ can be hydroxy, alkoxy, alkylamino, amino, or dialkylamino when twoof the group consisting of R²³, R²⁴, and R²⁶ are bonded to the same atomand that said Q^(b) group is bonded directly to a carbon atom;

[0207] R²³, R²⁴, R²⁵, and R²⁶ are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino,aminoalkyl, and hydroxyalkyl;

[0208] Q^(s) is selected from the group consisting of a single covalentbond and (CR³⁷R³⁸)_(b)—(W⁰)_(az) wherein az is an integer selected from0 through 1, b is an integer selected from 1 through 2, and W⁰ isselected from the group consisting of O, S, C(O), S(O)₂, N(R¹⁴), andON(R¹⁴) with the proviso that R¹⁴ is selected from other than halo whendirectly bonded to N and that (CR³⁷R³⁸)_(b) is bonded to E⁰;

[0209] R³⁷ and R³⁸ are independently selected from the group consistingof hydrido, halo, alkyl, and haloalkyl;

[0210] Y⁰ can be Q^(b)-Q^(ssss) wherein Q^(ssss) is (CH(R³⁸))^(r)—W⁵, ris an integer selected from 1 through 2, and W⁵ is selected from thegroup consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl,3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl,3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to lowest number substituent position of each W⁵ andthat (CH(R³⁸))_(r) is bonded to E⁰;

[0211] Y⁰ can be Q^(b)-Q^(ssssr) wherein Q^(ssssr) is (CH(R³⁸))_(r)—W⁶,r is an integer selected from 1 through 2, and W⁶ is selected from thegroup consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl,3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl,3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,⁶-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to highest number substituent position of each W⁶ andthat (CH(R³⁸))_(r) is bonded to E⁰.

[0212] In a more preferred embodiment of compounds of Formula I or apharmaceutically acceptable salt thereof,

[0213] J is selected from the group consisting of halo, hydroxy,hydroxyalkyl, amino, aminoalkyl, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ isselected from the group consisting of alkyl and haloalkyl;

[0214] B is selected from the group consisting of aryl and heteroarylwherein a carbon adjacent to the carbon at the point of attachment maybe substituted by R³², the other carbon adjacent to the carbon at thepoint of attachment may be substituted by R³⁶, a carbon adjacent to R³²and two atoms from the carbon at the point of attachment may besubstituted by R³³, a carbon adjacent to R³⁶ and two atoms from thecarbon at the point of attachment may be substituted by R³⁵, and anycarbon adjacent to both R³³ and R³⁵ may be substituted by R³⁴;

[0215] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, amidino, guanidino, dialkylsulfonium,carboxy, haloalkylthio, alkoxy,hydroxy, amino, alkoxyamino, thio, nitro,lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl,amidosulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl,haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl,carboxyalkyl, carboalkoxy, carboxamido, and cyano;

[0216] R³², R³³, R³⁴, R³⁵, and R³⁶ can independently be Q^(b);

[0217] B can be selected from the group consisting of C3-C8 alkyl C3-C8alkenyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl wherein each member ofgroup B may be optionally substituted at any carbon up to and including6 atoms from the point of attachment of B to A with one or more of thegroup consisting of R₃₂, R₃₃, R₃₄, R₃₅ and R₃₆;

[0218] B can be selected from the group consisting of C3-C10 cycloalkyl,C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9-partiallysaturated heterocyclyl, wherein each ring carbon may be optionallysubstituted with R₃₃, a ring carbon other than the ring carbon at thepoint of attachment of B to A may be optionally substituted with oxoprovided that no more than one ring carbon is substituted by oxo at thesame time, ring carbon and nitrogen atoms adjacent to the carbon atom atthe point of attachment may be optionally substituted with R₉ or R₁₃, aring carbon or nitrogen atom adjacent to the R₉ position and two atomsfrom the point of attachment may be substituted with R₁₀, a ring carbonor nitrogen atom adjacent to the R₁₃ position and two atoms from thepoint of attachment may be substituted with R₁₂, a ring carbon ornitrogen atom three atoms from the point of attachment and adjacent tothe R₁₀ position may be substituted with R₁₁, a ring carbon or nitrogenatom three atoms from the point of attachment and adjacent to the R₁₂position may be substituted with R₃₃, and a ring carbon or nitrogen atomfour atoms from the point of attachment and adjacent to the R₁₁ and R₃₃positions may be substituted with R₃₄;

[0219] R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independently selected from thegroup consisting of hydrido, amidino, guanidino, dialkylsulfonium,carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, thio,nitro, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl,amidosulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl,haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl,carboxyalkyl, carboalkoxy, carboxamido, and cyano;

[0220] A is selected from the group consisting of single covalent bond,(W⁷)_(rr)—(CH(R¹⁵))_(pa) and (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is aninteger selected from 0 through 1, pa is an integer selected from 0through 6, and W⁷ is selected from the group consisting of O, S, andC(O) with the proviso that no more than one of the group consisting ofrr and pa can be 0 at the same time;

[0221] R¹⁵ is selected from the group consisting of hydrido, hydroxy,halo, alkyl, and haloalkyl;

[0222] Ψ is NH;

[0223] X⁰ is hydrido;

[0224] R¹ is selected from the group consisting of hydrido, alkyl,alkoxy, alkylamino, alkylthio, haloalkylthio, haloalkyl, haloalkoxy, andhalo;

[0225] R² is Q, wherein Q is selected from the group consisting of aryland heteroaryl wherein a carbon adjacent to the carbon at the point ofattachment may be substituted by R⁹, the other carbon adjacent to thecarbon at the point of attachment may be substituted by R¹³, a carbonadjacent to R⁹ and two atoms from the carbon at the point of attachmentmay be substituted by R¹⁰, a carbon adjacent to R¹³ and two atoms fromthe carbon at the point of attachment may be substituted by R¹², and anycarbon adjacent to both R¹⁰ and R¹² may be substituted by R¹¹;

[0226] K is CR^(4a)R^(4b) wherein R^(4a) and R^(4b) are independentlyselected from the group consisting of halo and hydrido;

[0227] E⁰ is E¹, when K is CR^(4a)R^(4b), wherein E¹ is selected fromthe group consisting of a covalent single bond, C(O)N(H), (H)NC(O),S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0228] K can be (CH(R¹⁴))_(j)-T wherein j is selected from an integerfrom 0 through 1 and T is selected from the group consisting of singlecovalent bond and N(R⁷) with the proviso that (CH(R¹⁴))_(j) is bonded tothe phenyl ring;

[0229] R⁷ is selected from the group consisting of hydrido, hydroxy,alkyl, and alkoxyalkyl;

[0230] R¹⁴ is selected from the group consisting of hydrido and halo;

[0231] E⁰ is E², when K is (CH(R¹⁴))_(j)-T, wherein E² is selected fromthe group consisting of C(O)N(H), (H)NC(O), S(O)₂N(H), N(H)S(O)₂,S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0232] Y⁰ is formula (IV):

[0233] wherein D⁵, D⁶, J⁵, and J⁶ are independently selected from thegroup consisting of C, N, O, S and a covalent bond with the provisosthat no more than one can be a covalent bond, K² is independentlyselected from the group consisting of C, and N⁺, no more than one of D⁵,D⁶, J⁵ and J⁶ can be O, no more than one of D⁵, D⁶, J⁵, and J⁶ can be S,one of D⁵, D⁶, J⁵, and J⁶ must be a covalent bond when two of D⁵, D⁶,J⁵, and J⁶ are O and S, no more than three of D⁵, D⁶, J⁵, and J⁶ can beN when K² is N⁺, and no more than four of D⁵, D⁶, J⁵, and J⁶ can be Nwhen K² is carbon with the provisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are eachindependently selected to maintain the tetravalent nature of carbon,trivalent nature of nitrogen, the divalent nature of sulfur, and thedivalent nature of oxygen;

[0234] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, dialkylsulfonium, carboxy,haloalkylthio, alkoxy, hydroxy, amino, thio, nitro, lower alkylaminno,alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, alkenoyl,haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboalkoxy,carboalkoxyalkyl, and cyano;

[0235] Q^(b) is selected from the group consisting of NR²⁰R²¹,⁺NR²⁰R²¹R²², oxy, alkyl, alkylaminoalkyl, aminoalkyl,dialkylsulfoniumalkyl, and acylamino wherein R²⁰, R²¹, and R²² areindependently selected from the group consisting of hydrido, alkyl,hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkylwith the provisos that no more than one of R²⁰, R²¹, and R²² can behydroxy, alkoxy, alkylamino, amino, and dialkylamino and that R²⁰, R²¹,and R²² must be other than be hydroxy, alkoxy, alkylamino, amino, anddialkylamino when K² is N⁺;

[0236] Q^(b) can be selected from the group consisting ofdialkylsulfonium, trialkylphosphonium, C(NR²⁵)NR²³R²⁴,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴,and C(O)NR²³R²⁴ with the provisos that no more than one of R²³, R²⁴, andR²⁶ can be hydroxy, alkoxy, alkylamino, amino, or dialkylamino when twoof the group consisting of R²³, R²⁴, and R²⁶ are bonded to the same atomand that said Q^(b) group is bonded directly to a carbon atom;

[0237] R²³, R²⁴, R²⁵, and R²⁶ are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino,aminoalkyl, and hydroxyalkyl;

[0238] Q^(s) is selected from the group consisting of a single covalentbond and (CR³⁷R³⁸)_(b)—(W⁰)^(az) wherein az is an integer selected from0 through 1, b is the integer 1, and W⁰ is selected from the groupconsisting of O, S, and C(O) with the proviso that (CR³⁷R³⁸)_(b) isbonded to E⁰;

[0239] R³⁷ and R³⁸ are independently selected from the group consistingof hydrido, halo, alkyl, and haloalkyl.

[0240] In a specific embodiment of Formula I, compounds have the FormulaI-S:

[0241] or a pharmaceutically acceptable salt thereof, wherein;

[0242] J is selected from the group consisting of fluoro, chloro, bromo,hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, amino,aminomethyl, 1-aminoethyl, 2-aminoethyl, methoxy, ethoxy,trifluoromethoxy, N-methylamino, N-ethylamino, methythio, ethylthio, andtrifluorornethylthio;

[0243] B is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 1,2,4-triazol-3-yl,1,2,4-triazol-5-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl,1,3,4-oxadiazol-3-yl, 1,3,4-oxadiazol-5-yl, 3-isothiazolyl,5-isothiazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl,2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl,4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl,1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl,1,2,4-triazin-6-yl, and 1,2,3-triazin-4-yl, wherein a carbon adjacent tothe carbon at the point of attachment may be substituted by R³², theother carbon adjacent to the carbon at the point of attachment may besubstituted by R³⁶, a carbon adjacent to R³² and two atoms from thecarbon at the point of attachment may be substituted by R³³, a carbonadjacent to R³⁶ and two atoms from the carbon at the point of attachmentmay be substituted by R³⁵, and any carbon adjacent to both R³³, and R³⁵may be substituted by R³⁴;

[0244] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, amidino, guanidino, dimethylsulfonium,carboxy, methoxy,ethoxy, isopropoxy, propoxy, hydroxy, amino,methoxyamino, ethoxyamino, thio, nitro, aminomethyl, 1-aminoethyl,2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, methylthio,ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl,ethylsulfinyl, methylsulfonyl, ethylssulfonyl, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl,trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl,propanoyl, trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, cyano, and Q^(b);

[0245] B can be selected from the group consisting of 1-propenyl,propyl,isopropyl, butyl, 2-butenyl, 3-butenyl, 2-butynyl, sec-butyl, isobutyl,2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 4-pentenyl,2-pentynyl, 3-pentynyl, 2-pentyl, 1-methyl-2-butenyl,1-methyl-3-butenyl, 1-methyl-2-butenyl, 3-pentyl, 1-ethyl-2-propenyl,2-methylbutyl, 2-methyl-2-butenyl, 2-methyl-3-butenyl,2-methyl-3-butynyl, 3-methylbutyl, 3-methyl-2-butenyl,3-methyl-3-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl,2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl,1-methyl-3-pentenyl, 1-methyl-4-pentenyl, 1-methyl-2-pentynyl,1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl,1-propyl-2-propenyl, 1-ethyl-2-butynyl, 1-heptyl, 2-heptenyl,3-heptenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 2-heptynyl, 3-heptynyl,4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl,1-methyl-3-hexenyl, 1-methyl-4-hexenyl, 1-methyl-5-hexenyl,1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl,1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-4-pentenyl,1-butyl-2-propenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, l-octyl,2-octenyl, 3-octenyl, 4-octenyl, 5-octenyl, 6-octenyl, 7-octenyl,2-octynyl, 3-octynyl, 4-octynyl, 5-octynyl, 6-octynyl, 2-octyl,1-methyl-2-heptenyl, 1-methyl-3-heptenyl, 1-methyl-4-heptenyl,1-methyl-5-heptenyl, 1-methyl-6-heptenyl, 1-methyl-2-heptynyl,1-methyl-3-heptynyl, 1-methyl-4-heptenyl, 1-methyl-5-heptenyl,1-methyl-6-heptenyl, 1-methyl-2-heptenyl, 1-methyl-3-heptynyl,1-methyl-4-heptynyl, 1-methyl-5-heptynyl, 3-octyl, 1-ethyl-2-hexenyl,1-ethyl-3-hexenyl, 1-ethyl-4-hexenyl, 1-ethyl-2-hexynyl,1-ethyl-3-hexynyl, 1-ethyl-4-hexynyl, 1-ethyl-5-hexenyl,1-pentyl-2-propenyl, 4-octyl, 1-propyl-2-pentenyl, 1-propyl-3-pentenyl,1-propyl-4-pentenyl, 1-butyl-2-butenyl, 1-propyl-2-pentynyl,1-propyl-3-pentynyl, 1-butyl-2-butynyl, 1-butyl-3-butenyl,2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl,4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and3,3,3-trifluoropropyl, wherein each member of group B may be optionallysubstituted at any carbon up to and including 5 atoms from the point ofattachment of B to A with one or more of the group consisting of R₃₂,R₃₃, R₃₄, R₃₅, and R₃₆;

[0246] B can be selected from the group consisting of cyclopropyl,cyclobutyl, oxetan-2-yl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl,azetidin-3-yl, thiaetan-2-yl, thiaetan-3-yl, cyclopentyl,cyclopent-2-enyl, cyclopent-3-enyl, cyclohexyl, 4-methylcyclohexyl,4-chloro-3-ethylphenoxycyclohexyl, 3-trifluoromethoxyphenoxycyclohexyl,3-trifluoromethylcyclohexyl, 4-trifluoromethylcyclohexyl,3,5-bis-trifluoromethylcyclohexyl, adamantyl,3-trifluoromethyladamantyl, norbornyl, 3-trifluoromethylnorbomyl,norbornenyl, 7-oxabicyclo[2.2.1]heptan-2-yl, bicyclo[3.1.0]hexan-6-yl,cyclohex-2-enyl, cyclohex-3-enyl, cycloheptyl, cyclohept-2-enyl,cyclohept-3-enyl, cyclooctyl, cyclooct-2-enyl, cyclooct-3-enyl,cyclooctenyl, 2-morpholinyl, 3-morpholinyl, 4-morpholinyl,1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl,3-piperidinyl, 4-piperidinyl, l-pyrrolidinyl, 2-pyrrolidinyl,3-pyrrolidinyl, 2-dioxanyl, 2H-2-pyranyl, 2H-3-pyranyl, 2H-4-pyranyl,4H-2-pyranyl, 4H-3-pyranyl, 4H-4-pyranyl, 2H-pyran-2-one-3-yl,2H-pyran-2-one-4-yl, 2H-pyran-2-one-5-yl, 4H-pyranone-2-yl,4H-pyran-4-one-3-yl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl,2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl,2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein each ring carbonmay be optionally substituted with R³³, a ring carbon and nitrogen atomsadjacent to the carbon atom at the point of attachment may be optionallysubstituted with R₉ or R₁₃, a ring carbon or nitrogen atom adjacent tothe R₉ position and two atoms from the point of attachment may besubstituted with R₁₀, and a ring carbon or nitrogen atom adjacent to theR₁₃ position and two atoms from the point of attachment may besubstituted with R₁₂;

[0247] R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independently selected from thegroup consisting of amidino, guanidino, dimethylsulfonium,methylethylsulfonium, carboxy, methoxy, ethoxy, isopropoxy, propoxy,butoxy, hydroxy, amino, methoxyamino, ethoxyamino, aminomethyl,1-aminoethyl, 2-aminoethyl, N-N-dimethylamino, N-methylamino,N-ethylaminno, methylsulfinyl, ethylsulfinyl, methylsulfonyl,ethylsulfonyl, amidosulfonyl, N-methylamidosulfonyl,N,N-dimethylamidosulfonyl, acetyl, propanoyl, butanoyl, trifluoroacetyl,pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,2-carboxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl,N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

[0248] A is selected from the group consisting of single covalent bond,O, C(O), CH₂, CH₃CH, CF₃CH, CH₃CC(O), CF₃CC(O), C(O)CCH₃, C(O)CCF₃,CH₂C(O), (O)CCH₂, CH₂CH₂, CH₂CH₂CH₂, CH3CCH₂, CF₃CCH₂, CH₃CC(O)CH₂,CF₃CC(O)CH₂, CH₂C(O)CCH₃, CH₂C(O)CCF₃, CH₂CH₂C(O), and CH₂(O)CCH₂;

[0249] R¹ is selected from the group consisting of hydrido, methyl,ethyl, propyl, butyl, methoxy, ethoxy, propoxy, isopropoxy, butoxy,sec-butoxy, N-methylamino, N,N-dimethylamino, N-ethylamino,N,N-diethylamino, methylthio, ethylthio, isopropylthio,trifluoromethylthio, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;

[0250] R² is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 1,2,4-triazol-3-yl,1,2,4-triazol-5-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl,1,3,4-oxadiazol-3-yl, 1,3,4-oxadiazol-5-yl, 3-isothiazolyl,5-isothiazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl,2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl,4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl,1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl,1,2,4-triazin-6-yl, and 1,2,3-triazin-4-yl, wherein a carbon adjacent tothe carbon at the point of attachment may be substituted by R⁹, theother carbon adjacent to the carbon at the point of attachment may besubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment may be substituted by R¹⁰, a carbonadjacent to R¹³ and two atoms from the carbon at the point of attachmentmay be substituted by R¹², and any carbon adjacent to both R¹⁰ and R¹²may be substituted by R¹¹;

[0251] K is CR^(4a)R^(4b) wherein R^(4a) and R^(4b) are independentlyselected from the group consisting of chloro, fluoro, and hydrido;

[0252] E⁰ is E¹, when K is CR^(4a)R^(4b), wherein E¹ is selected fromthe group consisting of a covalent single bond, C(O)N(H), (H)NC(O),S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0253] K can be N(H) and CH₂N(H);

[0254] E⁰ is E², when K is N(H) and CH₂N(H), wherein E² is selected fromthe group consisting of C(O)N(H), (H)NC(O), S(O)₂N(H), N(H)S(O)₂,S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0255] Y⁰ is selected from the group of formulas consisting of:

[0256] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, dimethylsulfonium, carboxy,methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino,ethoxyamino, thio, nitro, aminomethyl, 1-aminoethyl, 2-aminoethyl,N-N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio,isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl,methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl, propanoyl,trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl,2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano;

[0257] Q^(b) is selected, when bonded to a carbon, from the groupconsisting of NR²⁰R²¹, ⁺NR²⁰R²¹R²², dimethylsulfonium,methylethylsulfonium, diethylsulfonium, trimethylphosphonium,C(NR²⁵)NR²³R²⁴, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴,and C(O)NR²³R²⁴ with the provisos that no more than one of R²⁰, R²¹, andR²² can be hydroxy, methoxy, ethoxy, N-methylamino, N,N-dimethylamino,and N,N,N-trimethylamino, and amino and that no more than one of R²³,R²⁴, and R²⁶ can be hydroxy, methoxy, ethoxy, N-methylamino,N,N-dimethylamino, N,N,N-trimethylamino, or amino when two of the groupconsisting of R²³, R²⁴, and R²⁶ are bonded to the same atom and thatsaid Q^(b) group is bonded directly to a carbon atom;

[0258] R²⁰, R²¹, R²², R²³, R²⁴, R²⁵, and R²⁶ are independently selectedfrom the group consisting of hydrido, methyl, ethyl, propyl, butyl,isopropyl, hydroxy, methoxy, ethoxy, isopropoxy, propoxy, 2-aminoethyl,2-(N-methylamino)ethyl, 2-(N,N-dimethylamino)ethyl,2-(N,N,N-trimethylamino)ethyl, N-(2-hydroxyethyl)amino,N,N-bis-(2-hydroxyethyl)amino, N-(2-hydroxyethyl)-N-(2-aminoethyl)amino,N-methylamino, N-ethylamino, N,N-dimethylamino, N,N-diethylamino, andN,N,N-trimethylamino;

[0259] Q^(b) is selected, when bonded to a nitrogen, from the groupconsisting of oxy, methyl, ethyl, 2-aminoethyl, 2-(N-methylamino)ethyl,2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl,N-(2-hydroxyethyl)amilno, N, N-bis-(2-hydroxyethyl)amino, amino,hydroxylamino, N-methoxyamino, N-methylamino, N,N-dimethylamino, andN,N,N-trimethylamino;

[0260] Q^(s) is selected from the group consisting of a single covalentbond, CH₂, CH₃CH, CF₂, CF₃CH, CH₂O, CH₃C(H)O, CF₃C(H)O, CH₂S, CH₃C(H)S,CF₃C(H)S, CH₂C(O), CH₃C(H)C(O), CF₃C(H)C(O), and CF₂C(O) with theproviso that Q^(s) is bonded to E⁰ through a carbon atom.

[0261] In a more preferred specific embodiment of Formula I, compoundshave the Formula I-MPS:

[0262] or a pharmaceutically acceptable salt thereof, wherein;

[0263] J is selected from the group consisting of fluoro, chloro,hydroxy, hydroxymethyl, amino, aminomethyl, methoxy, trifluoromethoxy,N-methylamino, methythio, and trifluoromethylthio;

[0264] B is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl,5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl,2-pyrimidinyl, 4-pyrimidinyl, Spyrimidinyl, 3-pyridazinyl,4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to thecarbon at the point of attachment may be substituted by R³², the othercarbon adjacent to the carbon at the point of attachment may besubstituted by R³⁶, a carbon adjacent to R³² and two atoms from thecarbon at the point of attachment may be substituted by R³³, a carbonadjacent to R³⁶ and two atoms from the carbon at the point of attachmentmay be substituted by R³⁵, and any carbon adjacent to both R³³ and R³⁵may be substituted by R³⁴;

[0265] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, amidino, guanidino, dimethylsulfonium,carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,methoxyamino, ethoxyamino, thio, nitro, aminomethyl, 1-aminoethyl,2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, methylthio,ethylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl,methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl, propanoyl,trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl,2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,2,2,2-tiffluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, cyano, and Q^(b);

[0266] B can be selected from the group consisting of 1-propenyl,propyl, isopropyl, butyl, 2-butenyl, 3-butenyl, sec-butyl, isobutyl,2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 4-pentenyl,2-pentyl, 1-methyl-2-butenyl, 1-methyl-3-butenyl, 3-pentyl,1-ethyl-2-propenyl, 2-methylbutyl, 2-methyl-2-butenyl,2-methyl-3-butenyl, 3-methylbutyl, 3-methyl-2-butenyl,3-methyl-3-butenyl, 2,2-difluoropropyl,2-trifluoromethyl-3,3,3-trifluoropropyl, 1,1,1,2,2,2-hexafluoropropyl,3,3,3-trifluoroprop-1-yl, and 3,3,3-trifluoroprop-2-yl, wherein eachmember of group B may be optionally substituted at any carbon up to andincluding 5 atoms from the point of attachment of B to A with one ormore of the group consisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆;

[0267] B can be selected from the group consisting of cyclopropyl,cyclobutyl, oxetan-2-yl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl,azetidin-3-yl, thiaetan-2-yl, thiaetan-3-yl, wherein each ring carbonmay be optionally substituted with R₃₃, a ring carbon and nitrogen atomsadjacent to the carbon atom at the point of attachment may be optionallysubstituted with R₉ or R₁₃, a ring carbon or nitrogen atom adjacent tothe R₉ position and two atoms from the point of attachment may besubstituted with R₁₀, and a ring carbon or nitrogen atom adjacent to theR₁₃ position and two atoms from the point of attachment may besubstituted with R₁₂;

[0268] R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independently selected from thegroup consisting of amidino, guanidino, dimethylsulfonium, carboxy,methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino,ethoxyamino, aminomethyl, 1-ainoethyl, 2-aminoethyl, N-N-methylamino,dimethylamino, N-ethylamino, methylsulfinyl, ethylsulfinyl,methylsulfonyl, ethylsulfonyl, amidosulfonyl, N-methylamidosulfonyl,N,N-dimethylamidosulfonyl, acetyl, propanoyl, trifluoroacetyl,pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano;

[0269] A is selected from the group consisting of single covalent bond,O, C(O), CH₂, CH₃CH, CF₃CH, CH₃CC(O), CF₃CC(O), C C(O)CCH₃, C(O)CCF₃,CH₂C(O), and (O)CCH₂;

[0270] R¹ is selected from the group consisting of hydrido, methyl,ethyl, propyl, methoxy, ethoxy, N-methylamino, dimethylamino,N-ethylamino, methylthio, ethylthio, trifluoromethylthio,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;

[0271] R² is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl,5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl,2-pyrimidinyl, 4-pyrimidinyl, Spyrimidinyl, 3-pyridazinyl,4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to thecarbon at the point of attachment may be substituted by R⁹, the othercarbon adjacent to the carbon at the point of attachment may besubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment may be substituted by R¹⁰, a carbonadjacent to R¹³ and two atoms from the carbon at the point of attachmentmay be substituted by R¹², and any carbon adjacent to both R¹⁰ and R¹²may be substituted by R¹¹;

[0272] K is CR^(4a)R^(4b) wherein R^(4a) and R^(4b) are independentlyselected from the group consisting of chloro, fluoro, and hydrido;

[0273] E₀ is E¹, when K is CR^(4a)R^(4b), wherein E¹ is selected fromthe group consisting of a covalent single bond, C(O)N(H), (H)NC(O),S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0274] K can be N(H) and CH₂N(H);

[0275] E⁰ is E2, when K is N(H) and CH₂N(H), wherein E² is selected fromthe group consisting of C(O)N(H), (H)NC(O), S(O)₂N(H), N(H)S(O)₂,S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0276] Y⁰ is selected from the group of formulas consisting of:

[0277] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, methoxy, ethoxy, isopropoxy,methylthio, ethylthio, trifluoromethylthio, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl,trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo,acetyl, propanoyl, trifluoroacetyl, pentafluoropropanoyl,methoxycarbonyl, ethoxycarbonyl, and cyano;

[0278] Q^(b) is selected, when bonded to a carbon, from the groupconsisting of NR²⁰R²¹, ⁺NR²⁰R²¹R²², dimethylsulfonium,methylethylsulfonium, diethylsulfonium, trimethylphosphonium,C(NR²⁵)NR²³R²⁴, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴,and C(O)NR²³R²⁴ with the provisos that no more than one of R²⁰, R²¹, andR²² can be hydroxy, methoxy, ethoxy, N-methylamino, N,N-dimethylamino,N,N,N-trimethylamino, or amino and that no more than one of R²³, R²⁴,and R²⁶ can be hydroxy, methoxy, ethoxy, N-methylamino,N,N-dimethylamino, N,N,N-trimethylamino, or amino when two of the groupconsisting of R²³, R²⁴, and R²⁶ are bonded to the same atom and thatsaid Q^(b) group is bonded directly to a carbon atom;

[0279] R²⁰, R²¹, R²², R²³, R²⁴, R²⁵, and R²⁶ are independently selectedfrom the group consisting of hydrido, methyl, ethyl, hydroxy, methoxy,ethoxy, 2-aminoethyl, 2-(N-methylamino)ethyl,2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl,N-(2-hydroxyethyl)amino, N,N-bis-(2-hydroxyethyl)amino,N-(2-hydroxyethyl)-N-(2-aminoethyl)amino, N-methylamino,N,N-dimethylamino, and N,N,N-trimethylamino;

[0280] Q^(b) is selected, when bonded to a nitrogen, from the groupconsisting of oxy, methyl, ethyl, 2-aminoethyl, 2-(N-methylamino)ethyl,2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl,N-(2-hydroxyethyl)amino, N,N-bis-(2-hydroxyethyl)amino, amino,hydroxylamino, N-methoxyamino, N-methylamino, N,N-dimethylamino, andN,N,N-trimethylamino;

[0281] Q^(s) is selected from the group consisting of a single covalentbond, CH₂, CH₃CH, CF₂, CF₃CH, CH₂O, CH₃C(H)O, CF₃C(H)O, CH₂S, CH₃C(H)S,CF₃C(H)S, CH₂C(O), CH₃C(H)C(O), CF₃C(H)C(O), and CF₂C(O) with theproviso that Q^(s) is bonded to E⁰ through a carbon atom.

[0282] In an even more preferred specific embodiment of compounds ofFormula I, compounds have the Formula I-EMPS:

[0283] or a pharmaceutically acceptable salt thereof, wherein;

[0284] J is selected from the group consisting of fluoro, chloro,hydroxy, hydroxymethyl, amino, aminomethyl, methoxy, trifluoromethoxy,and N-methylamino;

[0285] B is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl,5-isoxazolyl, 2-pyridyl, 3-pyridyl, and 4-pyridyl, wherein a carbonadjacent to the carbon at the point of attachment may be substituted byR³², the other carbon adjacent to the carbon at the point of attachmentmay be substituted by R³⁶, a carbon adjacent to R³² and two atoms fromthe carbon at the point of attachment may be substituted by R³³, acarbon adjacent to R³⁶, and two atoms from the carbon at the point ofattachment may be substituted by R³⁵, and any carbon adjacent to bothR³³ and R³⁵ may be substituted by R³⁴;

[0286] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, amidino, guanidino, methoxy, ethoxy,hydroxy, amino, methoxyamino, ethoxyamino, aminomethyl, 1-aminoethyl,2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, fluoro, chloro, bromo, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, methoxycarbonyl,ethoxycarbonyl, cyano, and Q^(b);

[0287] B can be selected from the group consisting of propyl, isopropyl,butyl, sec-butyl, isobutyl, 1-pentyl, 2-pentyl, 3-pentyl, 2-methylbutyl,3-methylbutyl, 2,2-difluoropropyl,2-trifluoromethyl-3,3,3-trifluoropropyl, 1,1,1,2,2,2-hexafluoropropyl,3,3,3-trifluoroprop-1-yl, and 3,3,3-trifluoroprop-2-yl, wherein eachmember of group B may be optionally substituted at any carbon up to andincluding 5 atoms from the point of attachment of B to A with one ormore of the group consisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆;

[0288] B can be selected from the group consisting of cyclopropyl,cyclobutyl, oxetan-2-yl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl,azetidin-3-yl, thiaetan-2-yl, thiaetan-3-yl, wherein each ring carbonmay be optionally substituted with R₃₃, a ring carbon and nitrogen atomsadjacent to the carbon atom at the point of attachment may be optionallysubstituted with R₉ or R₁₃, a ring carbon or nitrogen atom adjacent tothe R₉ position and two atoms from the point of attachment may besubstituted with R₁₀, and a ring carbon or nitrogen atom adjacent to theR₁₃ position and two atoms from the point of attachment may besubstituted with R₁₂;

[0289] R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independently selected from thegroup consisting of amidino, guanidino, carboxy, methoxy, ethoxy,hydroxy, amino, methoxyamino, ethoxyamino, aminomethyl, 1-aminoethyl,2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, acetyl,propanoyl, trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, carboxymethyl, methoxycarbonyl,ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano;

[0290] A is selected from the group consisting of single covalent bond,O, C(O), CH₂, CH₂C(O), and (O)CCH₂;

[0291] R¹ is selected from the group consisting of hydrido, methyl,ethyl, methoxy, ethoxy, N-methylamino, dimethylamino, N-ethylamino,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro,and bromo;

[0292] R² is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl,5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl,2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl,4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to thecarbon at the point of attachment may be substituted by R⁹, the othercarbon adjacent to the carbon at the point of attachment may besubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment may be substituted by R¹⁰, a carbonadjacent to R¹³ and two atoms from the carbon at the point of attachmentmay be substituted by R¹², and any carbon adjacent to both R¹⁰, and R¹²may be substituted by R¹¹;

[0293] K is CR^(4a)R^(4b) wherein R^(4a) and R^(4b) are independentlyselected from the group consisting of chloro, fluoro, and hydrido;

[0294] E⁰ is E¹, when K¹ is CR^(4a)R^(4b), wherein E¹ is selected fromthe group consisting of a covalent single bond, C(O)N(H), (H)NC(O),S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0295] K can be N(H) and CH₂N(H);

[0296] E⁰ is E², when K is N(H) and CH₂N(H), wherein E² is selected fromthe group consisting of C(O)N(H), (H)NC(O), S(O)₂N(H), N(H)S(O)₂,S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0297] Y⁰ is selected from the group of formulas consisting of:

[0298] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, methoxy, ethoxy, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro,chioro, bromo, acetyl, trifluoroacetyl, methoxycarbonyl, ethoxycarbonyl,and cyano;

[0299] Q^(b) is selected from the group consisting of NR²⁰R²¹,⁺NR²⁰R²¹R²², dimethylsulfonium, methylethylsulfonium, diethylsulfonium,timethyiphosphonium, C(NR²⁵)NR²³R²⁴, N(R²⁶)C(NR²⁵)N(R23)(R²⁴),C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with theprovisos that no more than one of R²⁰, R²¹, and R²² can be hydroxy,methoxy, ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino,or amino and that no more than one of R²³, R²⁴, and R²⁶ can be hydroxy,methoxy, ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino,or amino when two of the group consisting of R²³, R²⁴, and R²⁶ arebonded to the same atom and that said Q^(b) group is bonded directly toa carbon atom;

[0300] R²⁰, R²¹, R²², R²³, R²⁴, R²⁵, and R²⁶ are independently selectedfrom the group consisting of hydrido, methyl, ethyl, hydroxy, methoxy,ethoxy, 2-aminoethyl, 2-(N-methylamino)ethyl,2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl,N-(2-hydroxyethyl)amino, N,N-bis-2-hydroxyethyl)amino,N-(2-hydroxyethyl)-N-(2-aminoethylamino, N-methylamino,N,N-dimethylamino, and N,N,N-trimethylamino;

[0301] Q^(s) is selected from the group consisting of a single covalentbond, CH₂, CH₃CH, CF₂, CF₃CH, CH₂O, CH₃C(H)O, CF₃C(H)O, CH₂C(O),CH₃C(H)C(O), CF₃C(H)C(O), and CF₂C(O) with the proviso that Q^(s) isbonded to E⁰ through a carbon atom.

[0302] In another preferred embodiment of a compound of Formula I, saidcompound is the Formula:

[0303] or a phanmaceutically acceptable salt thereof, wherein;

[0304] J is selected from the group consisting of halo, haloalkyl,hydroxy, hydroxyalkyl, amino, aminoalkyl, amidino, carboxy, carboxamido,alkylsulfinyl, acyl, cyano, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ is alkylor haloalkyl;

[0305] B is phenyl or a heteroaryl of 5 or 6-ring members, wherein anitrogen with a removable hydrogen or a carbon adjacent to the carbon atthe point of attachment of said phenyl or heteroaryl ring to A isoptionally substituted by R³², a nitrogen with a removable hydrogen or acarbon at the other position adjacent to the point of attachment isoptionally substituted by R³⁶, a nitrogen with a removable hydrogen or acarbon adjacent to R³² and two atoms from the point of attachment isoptionally substituted by R³³, a nitrogen with a removable hydrogen or acarbon adjacent to R³⁶ and two atoms from the point of attachment isoptionally substituted by R³⁵, and a nitrogen with a removable hydrogenor a carbon adjacent to both R³³ and R³⁵ is optionally substituted byR³⁴;

[0306] R⁹, R¹⁰, R¹¹, R¹², R¹³, R³², R³³, R³⁴, R³⁵, and R³⁶ areindependently selected from the group consisting of hydrido, acetamido,haloacetamido, amidino, guanidino, alkylenedioxy, haloalkylthio,alkanoyloxy, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy,heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy,alkoxyalkyl, haloalkoxylalkyl, hydroxy, amino, alkoxyamino, nitro,alkylamino, N-alkyl-N-arylamino, arylamino, aralkylamino,heteroarylamino, heteroaralkylamino, heterocyclylamino,heterocyclylalkylamino, alkylthio, alkylthioalkyl, alkylsulfinyl,arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl,alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl,heteroarylsulfonyl, alkylsulfonylalkyl, aryl, aralkyl, cycloalkyl,cycloalkylalkyl, heteroaryl, heterocyclyl, alkylsulfonamido,amidosulfonyl, alkanoyl, haloalkanoyl, alkyl, alkenyl, halo, haloalkyl,haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl,haloalkoxyalkyl, carboxyalkyl, carboalkoxy, carboxy, carboxamido,carboxamidoalkyl, and cyano;

[0307] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently optionally Q^(b);

[0308] B is optionally selected from the group consisting of hydrido,trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8alkynyl, and C2-C8 haloalkyl, wherein each member of group B isoptionally substituted at any carbon up to and including 6 atoms fromthe point of attachment of B to A with one or more of the groupconsisting of R³², R³³, R³⁴, R³⁵, and R³⁶;

[0309] B is optionally a C3-C12-cycloalkyl or C4-C9 saturatedheterocyclyl, wherein each ring carbon is optionally substituted withR³³, a nng carbon other than the ring carbon at the point of attachmentof B to A is optionally substituted with oxo provided that no more thanone ring carbon is substituted by oxo at the same time, ring carbons anda nitrogen adjacent to the carbon atom at the point of attachment areoptionally substituted with R⁹ or R¹³, a ring carbon or nitrogen atomadjacent to the R⁹ position and two atoms from the point of attachmentis optionally substituted with R¹⁰, a ring carbon or nitrogen adjacentto the R¹³ position and two atoms from the point of attachment isoptionally substituted with R¹², a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹⁰ position isoptionally substituted with R¹¹, a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹² position isoptionally substituted with R³³, and a ring carbon or nitrogen fouratoms from the point of attachment and adjacent to the R¹¹ and R³³positions is optionally substituted with R³⁴;

[0310] A is selected from the group consisting of a bond,(W⁷)_(rr)—(CH(R¹⁵))_(pa), and (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is 0or 1, pa is an integer selected from 0 through 6, and W⁷ is selectedfrom the group consisting of O, S, C(O), (R⁷)NC(O), (R⁷)NC(S), and N(R⁷)with the proviso that no more than one of the group consisting of rr andpa is 0 at the same time and with the further proviso that W⁷ isselected from other than C(O) when W⁷ is bonded to Ψ;

[0311] R⁷ is selected from the group consisting of hydrido, hydroxy, andalkyl;

[0312] R¹⁵ is selected from the group consisting of hydrido, hydroxy,halo, alkyl, and haloalkyl;

[0313] Ψ is NH or NOH;

[0314] X⁰ and R¹ are independently selected from the group consisting ofhydrido, alkyl, alkenyl, cyano, halo, haloalkyl, haloalkoxy,haloalkylthio, amino, aminoalkyl, alkylamino, amidino, hydroxy,hydroxyamino, alkoxy, hydroxyalkyl, alkoxyamino, thiol, and alkylthio;

[0315] R² is Z⁰-Q;

[0316] Z⁰ is selected from the group consisting of a bond, (CR⁴¹R⁴²)_(q)wherein q is an integer selected from 1 through 3, and(CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p) wherein g and p are integersindependently selected from 0 through 3 and W⁰ is selected from thegroup consisting of O, S, C(O), S(O), N(R⁴¹), and ON(R⁴¹);

[0317] Z⁰ is optionally (CH(R⁴¹))_(e)—W²²—(CH(R⁴²)_(h) wherein e and hare independently 0 or 1 and W²² is selected from the group consistingof CR⁴¹═CR⁴², 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl,1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl,2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl,1,2-piperazinyl, 1,3-piperazinyl, 2,3-piperazinyl, 2,6-piperazinyl,1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl,2,6-piperidinyl, 3,4-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl,2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl,2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, and3,4-tetrahydrofuranyl, wherein Z⁰ is directly bonded to the benzene ringand W²² is optionally substituted with one or more substituents selectedfrom the group consisting of R⁹, R¹⁰, R¹¹, R¹², and R¹³;

[0318] R⁴¹ and R⁴² are independently selected from the group consistingof amidino, hydroxyamino, hydrido, hydroxy, amino, and alkyl;

[0319] Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein anitrogen with a removable hydrogen or a carbon adjacent to the carbon atthe point of attachment of said phenyl or heteroaryl ring to Z⁰ isoptionally substituted by R⁹, a nitrogen with a removable hydrogen or acarbon at the other position adjacent to the point of attachment isoptionally substituted by R¹³, a nitrogen with a removable hydrogen or acarbon adjacent to R⁹ and two atoms from the point of attachment isoptionally substituted by R¹⁰, a nitrogen with a removable hydrogen or acarbon adjacent to R¹³ and two atoms from the point of attachment isoptionally substituted by R¹², and a nitrogen with a removable hydrogenor a carbon adjacent to both R¹⁰ and R¹² is optionally substituted byR¹¹;

[0320] Q is optionally hydrido with the proviso that Z⁰ is selected fromother than a bond;

[0321] K is CR^(4a)R^(4b);

[0322] R^(4a) and R^(4b) are independently selected from the groupconsisting of halo, hydrido, hydroxy, alkyl, and haloalkyl;

[0323] E⁰, with the proviso that K is CR^(4a)R^(4b) is E¹ wherein E¹ isselected from the group consisting of a covalent single bond, C(O)N(H),(H)NC(O), C(S)N(H), (H)NC(S), S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), andC(O)N(H)S(O)₂;

[0324] K is optionally (CH(R¹⁴))_(j)-T wherein j is 0 or 1 and T is abond or N(R⁷) with the proviso that (CH(R¹⁴))_(j) is bonded to thephenyl ring;

[0325] R¹⁴ is selected from the group consisting of hydrido, halo,alkyl, and haloalkyl;

[0326] E⁰, with the proviso that K is (CH(R¹⁴))_(j)-T, is E² wherein E²is selected from the group consisting of C(O)N(H), (H)NC(O), C(S)N(H),(H)NC(S), S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0327] Y⁰ is phenyl or a heteroaryl of 5 or 6 ring members, wherein onecarbon of said phenyl or said heteroaryl is substituted by Q^(s), acarbon two or three contiguous atoms from the point of attachment ofQ^(s) to said phenyl or said heteroaryl to said phenyl or saidheteroaryl is substituted by Q^(b), a carbon adjacent to the point ofattachment of Q^(s) is optionally substituted by R¹⁷; another carbonadjacent to the point of attachment of Q^(s) is optionally substitutedby R¹⁸, a carbon adjacent to Q_(b) is optionally substituted by R¹⁶, andanother carbon adjacent to Q^(b) is optionally substituted by R¹⁹;

[0328] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, haloalkylthio,alkoxy, hydroxy, amino, nitro, alkoxyamino, alkylamino, alkylthio,alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, alkenyl,halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, haloalkoxyalkyl,carboalkoxy, and cyano;

[0329] R¹⁶ or R¹⁹ is optionally selected from the group consisting ofNR²⁰R²¹, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴) and C(NR²⁵)NR²³R²⁴ with the provisothat R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0330] Q^(b) is selected from the group consisting of NR²⁰R²¹,aminoalkyl, hydrido, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, withthe proviso that no more than one of R²⁰ and R²¹ is selected from thegroup consisting of hydroxy, amino, alkylamino, and dialkylamino at thesame time, with the further proviso that no more than one of R²³ and R²⁴is selected from the group consisting of hydroxy, amino, alkylamino, anddialkylamino at the same time;

[0331] R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ are independently selected fromthe group consisting of hydrido, alkyl, hydroxy, aminoalkyl, amino,dialkylamino, alkylamino, and hydroxyalkyl;

[0332] Q^(s) is selected from the group consisting of a bond,(CR³⁷R³⁸)_(b) wherein b is an integer selected from 1 through 4, and(CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 3 and W¹ is selected from thegroup consisting of C(O)N(R¹⁴), (R¹⁴)NC(O), S(O), S(O)₂, S(O)₂N(R¹⁴),N(R¹⁴)S(O)₂, and N(R¹⁴), with the proviso that R¹⁴ is selected fromother than halo when directly bonded to N, and with the additionalproviso that (CR³⁷R³⁸)_(b) and (CH(R¹⁴))_(c) are bonded to E⁰;

[0333] R³⁷ and R³⁸ are independently selected from the group consistingof hydrido, alkyl, and haloalkyl;

[0334] R³⁸ is optionally aroyl or heteroaroyl, wherein R³⁸ is optionallysubstituted with one or more substituents selected from the groupconsisting of R¹⁶, R¹⁷, R¹⁸, and R¹⁹;

[0335] Y⁰ is optionally Y^(AT) wherein Y^(AT) is Q^(b)-Q^(s);

[0336] Y⁰ is optionally Q^(b)-Q^(s) wherein Q^(ss) is(CH(R¹⁴))_(e)—W²—(CH(R¹⁵))^(h) wherein e and h are independently 1 or 2and W² is CR^(4a)═CR^(4b), with the proviso that (CH(R¹⁴))_(e) is bondedto E⁰.

[0337] In another more preferred embodiment of a compound of Formula I,said compound is the Formula:

[0338] or a pharmaceutically acceptable salt thereof, wherein;

[0339] J is selected from the group consisting of halo, haloalkyl,hydroxy, hydroxyalkyl, amino, aminoalkyl, amidino, carboxy, carboxamido,alkylsulfinyl, formyl, cyano, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ is alkylor haloalkyl;

[0340] B is phenyl or a heteroaryl of 5 or 6 ring members, wherein acarbon adjacent to the carbon at the point of attachment of said phenylor heteroaryl ring to A is optionally substituted by R³², the othercarbon adjacent to the carbon at the point of attachment is optionallysubstituted by R³⁶, a carbon adjacent to R³² and two atoms from thecarbon at the point of attachment is optionally substituted by R³³, acarbon adjacent to R³⁶ and two atoms from the carbon at the point ofattachment is optionally substituted by R³⁵, and any carbon adjacent toboth R³³ and R³⁵ is optionally substituted by R³⁴;

[0341] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkylenedioxy, haloalkylthio, alkanoyloxy, alkoxy, hydroxy,amino, alkoxyamino, haloalkanoyl, nitro, alkylamino, alkylthio, aryl,aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl,alkylsulfonamido, amidosulfonyl, alkyl, alkenyl, halo, haloalkyl,haloalkenyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl,carboalkoxy, carboxy, carboxamido, cyano, and Q^(b);

[0342] B is optionally selected from the group consisting of hydrido,trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8alkynyl, and C2-C8 haloalkyl, wherein each member of group B isoptionally substituted at any carbon up to and including 6 atoms fromthe point of attachment of B to A with one or more of the groupconsisting of R³², R³³, R³⁴, R³⁵, and R³⁶;

[0343] B is optionally a C3-C12 cycloalkyl or a C4-C9 saturatedheterocyclyl, wherein each ring carbon is optionally substituted withR³³, a ring carbon other than the ring carbon at the point of attachmentof B to A is optionally substituted with oxo provided that no more thanone ring carbon is substituted by oxo at the same time, ring carbons anda nitrogen adjacent to the carbon atom at the point of attachment areoptionally substituted with R⁹ or R¹³, a ring carbon or nitrogen atomadjacent to the R⁹ position and two atoms from the point of attachmentis optionally substituted with R¹⁰, a ring carbon or nitrogen atomadjacent to the R¹³ position and two atoms from the point of attachmentis optionally substituted with R¹², a ring carbon or nitrogen atom threeatoms from the point of attachment and adjacent to the R¹⁰ position isoptionally substituted with R¹¹, a ring carbon or nitrogen atom threeatoms from the point of attachment and adjacent to the R¹² position isoptionally substituted with R³³, and a ring carbon or nitrogen atom fouratoms from the point of attachment and adjacent to the R¹¹ and R³³positions is optionally substituted with R³⁴;

[0344] R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, alkoxyamino,alkanoyl, haloalkanoyl, amidino, guanidino, alkylenedioxy,haloalkylthio, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy,heteroaryloxy, heteroaralkoxy,heterocyclyloxy, heterocyclylalkoxy,hydroxy, amino, alkylamino, N-alkyl-N-arylamino, arylamino,aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino,heterocyclylalkylamino, alkylthio, alkylsulfinyl, arylsulfinyl,aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfamido,alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl,heteroarylsulfonyl, amidosulfonyl, alkyl, aryl, aralkyl, cycloalkyl,cycloalkylalkyl, heteroaryl, heterocyclyl, halo, haloalkyl, haloalkoxy,hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy,carboxyalkyl, carboxamido, and cyano;

[0345] A is bond or (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is 0 or 1, pa isan integer selected from 0 through 3, and W⁷ is selected from the groupconsisting of O, S, C(O), (R⁷)NC(O), (R⁷)NC(S), and N(R⁷), with thefurther proviso that W⁷ is selected from other than C(O) when W⁷ isbonded to the N(H) on the benzene ring;

[0346] R⁷ is selected from the group consisting of hydrido, hydroxy andalkyl;

[0347] R¹⁵ is selected from the group consisting of hydrido, hydroxy,halo, alkyl, and haloalkyl;

[0348] R¹ and X⁰ is selected from the group consisting of hydrido,alkyl, cyano, halo, haloalkyl, haloalkoxy, amino, aminoalkyl,alkylamino, amidino, hydroxy, hydroxyamino, alkoxy, hydroxyalkyl,alkoxyamino, thiol, and alkylthio;

[0349] R² is Z⁰-Q;

[0350] Z⁰ is selected from the group consisting of a bond, (CR⁴¹R⁴²)_(q)wherein q is 1 or 2, and (CH(R⁴¹))_(g)—W —(CH(R⁴²))_(p) wherein g and pare integers independently selected from 0 through 3 and W⁰ is selectedfrom the group consisting of O, S, C(O), S(O), N(R⁴¹), and ON(R⁴¹);

[0351] Z⁰ is optionally (CH(R⁴¹))_(e)—W²²—(CH(R⁴²))_(h) wherein e and hare independently 0 or 1 and W²² is selected from the group consistingof CR⁴¹═CR⁴², 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl,1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl,2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl,1,2-piperazinyl, 1,3-piperazinyl, 2,3-piperazinyl, 2,6-piperazinyl,1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl,2,6-piperidinyl, 3,4-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl,2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl,2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, and3,4-tetrahydrofuranyl, wherein Z⁰ is directly bonded to the benzene ringand W²² is optionally substituted with one or more substituents selectedfrom the group consisting of R⁹, R¹⁰, R¹¹, R¹², and R¹³;

[0352] R⁴¹ and R⁴² are independently selected from the group consistingof hydrido, hydroxy, and amino;

[0353] Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein acarbon adjacent to the carbon at the point of attachment of said phenylor heteroaryl ring to Z⁰ is optionally substituted by R⁹, the othercarbon adjacent to the carbon at the point of attachment is optionallysubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹⁰, acarbon adjacent to R¹³ and two atoms from the carbon at the point ofattachment is optionally substituted by R¹², and any carbon adjacent toboth R¹⁰ and R¹² is optionally substituted by R¹¹;

[0354] Q is optionally hydrido with the proviso that Z⁰ is other than abond;

[0355] K is CR^(4a)R^(4b);

[0356] R^(4a) and R^(4b) are independently selected from the groupconsisting of halo, hydrido, and hydroxy;

[0357] E⁰, with the proviso that K is CR^(4a)R^(4b), is E¹ wherein E¹ isselected from the group consisting of a covalent single bond, C(O)N(H),(H)NC(O), S(O)₂N(H), and N(H)S(O)₂;

[0358] K is optionally (CH(R¹⁴))_(j)-T wherein j is 0 or 1 and T is abond or N(R⁷) with the proviso that (CH(R¹⁴))_(j) is bonded to thephenyl ring;

[0359] R¹⁴ is hydrido or halo;

[0360] E⁰, with the proviso that K is (CH(R¹⁴))_(j)-T, is E² wherein E²is selected from the group consisting of C(O)N(H), (H)NC(O), C(S)N(H),(H)NC(S), S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂;

[0361] Y⁰ is phenyl or a heteroaryl of 5 or 6 ring members, wherein onecarbon of said phenyl or said heteroaryl is substituted by Q^(s), acarbon two or three atoms from the point of attachment of Q^(s) to saidphenyl or said heteroaryl is substituted by Q^(b), a carbon adjacent tothe point of attachment of Q^(s) is optionally substituted by R¹⁷,another carbon adjacent to the point of attachment of Q^(s) isoptionally substituted by R¹⁸, a carbon adjacent to Q^(b) is optionallysubstituted by R¹⁶, and another carbon adjacent to Q^(b) is optionallysubstituted by R¹⁹;

[0362] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, haloalkylthio,alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio,alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo,haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

[0363] R¹⁶ or R¹⁹ is optionally selected from the group consisting ofNR²⁰R²¹, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the provisothat R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0364] Q is selected from the group consisting of NR²⁰R²¹, hydrido,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the proviso that nomore than one of R²⁰ and R²¹ is selected from the group consisting ofhydroxy, amino, alkylamino, and dialkylamino at the same time, with thefurther proviso that no more than one of R²³ and R²⁴ is selected fromthe group consisting of hydroxy, amino, alkylamino, and dialkylamino atthe same time;

[0365] R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ are independently selected fromthe group consisting of hydrido, alkyl, hydroxy, amino, alkylamino anddialkylamino;

[0366] Q^(s) is selected from the group consisting of a bond,(CR³⁷R³⁸)_(b) wherein b is an integer selected from 1 through 4, and(CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 3 and W¹ is selected from thegroup consisting of C(O)N(R¹⁴), (R¹⁴)NC(O), S(O), S(O)₂, S(O)₂N(R¹⁴),N(R¹⁴)S(O)₂, and N(R¹⁴), with the proviso that R¹⁴ is selected fromother than halo when directly bonded to N, and with the additionalproviso that (CR³⁷R³⁸)_(b) and (CR³⁷R³⁸)_(b), and (CH(R¹⁴))_(c) arebonded to E⁰;

[0367] R³⁷ and R³⁸ are independently selected from the group consistingof hydrido, alkyl, and haloalkyl;

[0368] R³⁸ is optionally aroyl or heteroaroyl, wherein R³⁸ is optionallysubstituted with one or more substituents selected from the groupconsisting of R¹⁶, R¹⁷, R¹⁸, and R¹⁹;

[0369] Y⁰ is optionally Y^(AT) wherein Y^(AT) is Q^(b)-Q^(s);

[0370] Y⁰ is optionally Q^(b)-Q^(ss) wherein Q^(ss) is(CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h), wherein e and h are independently 1 or 2and W² is CR^(4a)═CR^(4b) with the proviso that (CH(R¹⁴))_(e) is bondedto E⁰.

[0371] In another even more preferred embodiment of a compound ofFormula I, said compound is the Formula:

[0372] or a pharmaceutically acceptable salt thereof, wherein;

[0373] B is phenyl or heteroaryl of 5 or 6 members, wherein a carbonadjacent to the carbon at the point of attachment is optionallysubstituted by R³², the other carbon adjacent to the carbon at the pointof attachment is optionally substituted by R³⁶, a carbon adjacent to R³²and two atoms from the carbon at the point of attachment is optionallysubstituted by R³³, a carbon adjacent to R³⁶ and two atoms from thecarbon at the point of attachment is optionally substituted by R³⁵, andany carbon adjacent to both R³³ and R³⁵ is optionally substituted byR³⁴;

[0374] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio,amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl,hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q^(b);

[0375] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, haloalkylthio,alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl,alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl,haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

[0376] R¹⁶ or R¹⁹ is optionally NR²⁰R²¹ or C(NR²⁵)NR²³R²⁴, with theproviso that R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0377] Q^(b) is selected from the group consisting of NR²⁰R²¹, hydrido,and C(NR²⁵)NR²³R²⁴, with the provisos that no more than one of R²⁰ andR²¹ is hydroxy at the same time and that no more than one of R²³ and R²⁴is hydroxy at the same time;

[0378] R²⁰, R²¹, R²³, R²⁴, and R²⁵ are independently selected from thegroup consisting of hydrido, alkyl, and hydroxy.

[0379] In still another even more preferred embodiment of a compound ofFormula I, said compound is the Formula:

[0380] or a pharmaceutically acceptable salt thereof, wherein;

[0381] B is selected from the group consisting of hydrido, C2-C8 alkyl,C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each memberof group B is optionally substituted at any carbon up to and including 6atoms from the point of attachment of B to A with one or more of thegroup consisting of R³², R³³, R³⁴, R³⁵, and R³⁶;

[0382] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio,amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl,hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q^(b);

[0383] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, haloalkylthio,alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl,alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl,haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

[0384] R¹⁶ or R¹⁹ is optionally selected from the group consisting ofNR²⁰R²¹, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the provisothat R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0385] Q^(b) is selected from the group consisting of NR²⁰R²¹, hydrido,C(NR²⁵)NR²³R²⁴, and N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), with the provisos that nomore than one of R²⁰ and R²¹ is hydroxy at the same time and that nomore than one of R²³ and R²⁴ is hydroxy at the same time;

[0386] R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ are independently selected fromthe group consisting of hydrido, alkyl, and hydroxy.

[0387] In an additional even more preferred embodiment of a compound ofFormula I, said compound is the Formula:

[0388] or a pharmaceutically acceptable salt thereof, wherein;

[0389] B is a C3-C7 cycloalkyl or a C4-C6 saturated heterocyclyl,wherein each ring carbon is optionally substituted with R³³, a ringcarbon other than the ring carbon at the point of attachment of B to Ais optionally substituted with oxo provided that no more than one ringcarbon is substituted by oxo at the same time, ring carbons and anitrogen adjacent to the carbon atom at the point of attachment areoptionally substituted with R⁹ or R¹³, a ring carbon or nitrogenadjacent to the R⁹ position and two atoms from the point of attachmentis optionally substituted with R¹⁰, a ring carbon or nitrogen adjacentto the R¹³ position and two atoms from the point of attachment isoptionally substituted with R¹², a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹⁰ position isoptionally substituted with R¹¹, a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹² position isoptionally substituted with R³³, and a ring carbon or nitrogen fouratoms from the point of attachment and adjacent to the R¹¹ and R³³positions is optionally substituted with R³⁴;

[0390] R³³ and R³⁴ are independently selected from the group consistingof hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy,hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl,alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl,carboalkoxy, carboxy, carboxamido, and cyano;

[0391] R³³ is optionally Q^(b);

[0392] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, haloalkylthio,alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl,alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl,haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

[0393] R¹⁶ or R¹⁹ is optionally NR²⁰R²¹ or and C(NR²⁵)NR²³R²⁴, with theproviso that R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0394] Q is selected from the group consisting of NR²⁰R²¹, hydrido, andC(NR²⁵)NR²³R²⁴, with the provisos that no more than one of R²⁰ and R²¹is hydroxy at the same time and that no more than one of R²³ and R²⁴ ishydroxy at the same time;

[0395] R²⁰, R²¹, R²³, R²⁴, and R²⁵ are independently selected from thegroup consisting of hydrido, alkyl, and hydroxy.

[0396] The three groups of even more preferred embodiment compounds ofthe present invention described above and having the Formula:

[0397] or a pharmaceutically acceptable salt thereof, have commonstructural units, wherein;

[0398] J is selected from the group consisting of halo, haloalkyl,hydroxy, hydroxyalkyl, amino, aminoalkyl, cyano, O—R⁶, NH—R⁶, and S—R⁶,wherein R⁶ is alkyl or haloalkyl;

[0399] R⁹, R¹¹, and R¹³ are independently selected from the groupconsisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino,alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl,amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl,hydroxyhaloalkyl, carboxy, carboxamido, and cyano;

[0400] R¹⁰ and R¹² are independently selected from the group consistingof hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, aryl,aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy,cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy,heteroaralkoxy,heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino,alkoxyamino, alkylamino, arylamino, aralkylamino, heteroarylamino,heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino,alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl,cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl,cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl,aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo,haloalkyl, and cyano;

[0401] A is a single covalent bond or (CH(R¹⁵))_(pa)—(W⁷)_(rr) whereinrr is 0 or 1, pa is an integer selected from 0 through 3, and W⁷ is(R⁷)NC(O) or N(R⁷);

[0402] R⁷ is selected from the group consisting of hydrido, hydroxy andalkyl;

[0403] R¹⁵ is selected from the group consisting of hydrido, halo,alkyl, and haloalkyl;

[0404] R¹ and X⁰ are independently selected from the group consisting ofhydrido, hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl,alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino,haloalkyl, haloalkoxy, and halo;

[0405] R² is Z⁰-Q;

[0406] Z⁰ is selected from the group consisting of a covalent singlebond, CH₂, CH₂CH₂, W⁰—(CH(R⁴²))_(p) wherein p is 0 or 1 and W⁰ isselected from the group consisting of O, S, and N(R⁴¹);

[0407] R⁴¹ and R⁴² are independently hydrido or alkyl;

[0408] Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein acarbon adjacent to the carbon at the point of attachment is optionallysubstituted by R⁹ the other carbon adjacent to the carbon at the pointof attachment is optionally substituted by R¹³, a carbon adjacent to R⁹and two atoms from the carbon at the point of attachment is optionallysubstituted by R¹⁰, a carbon adjacent to R¹³ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹², andany carbon adjacent to both R¹⁰ and R¹² is optionally substituted byR¹¹;

[0409] Y⁰ is phenyl or a heteroaryl of 5 or 6 ring members, wherein onecarbon of said phenyl or said heteroaryl is substituted by Q^(s), acarbon two or three contiguous atoms from the point of attachment ofQ^(s) is substituted by Q^(b), a carbon adjacent to the point ofattachment of Q^(s) is optionally substituted by R¹⁷, another carbonadjacent to the point of attachment of Q^(s) is optionally substitutedby R¹⁸, a carbon adjacent to Q^(b) is optionally substituted by R¹⁶; andanother carbon adjacent to Q^(b) is optionally substituted by R¹⁹;

[0410] Q^(s) is selected from the group consisting of a single covalentbond, CH₂, and CH₂CH₂.

[0411] In a fourth group of an even more preferred embodiment of acompound of Formula I, said compound is the Formula:

[0412] or a pharmaceutically acceptable salt thereof, have commonstructural units, wherein;

[0413] J is selected from the group consisting of halo, haloalkyl,hydroxy, hydroxyalkyl, amino, aminoalkyl, cyano, O—R⁶, NH—R⁶, and S—R⁶,wherein R⁶ is alkyl or haloalkyl;

[0414] B is phenyl or a heteroaryl of 5 or 6 ring members, wherein acarbon adjacent to the carbon at the point of attachment is optionallysubstituted by R³², the other carbon adjacent to the carbon at the pointof attachment is optionally substituted by R³⁶, a carbon adjacent to R³²and two atoms from the carbon at the point of attachment is optionallysubstituted by R³³, a carbon adjacent to R³⁶ and two atoms from thecarbon at the point of attachment is optionally substituted by R³⁵, andany carbon adjacent to both R³³ and R³⁵ is optionally substituted byR³⁴;

[0415] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkylenedioxy, haloalkylthio, alkanoyloxy, alkoxy, hydroxy,amino, alkoxyamino, haloalkanoyl, nitro, alkylamino, alkylthio, aryl,aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl,alkylsulfonamido, amidosulfonyl, alkyl, alkenyl, halo, haloalkyl,haloalkenyl, haloalkoxy, hydroxyalkyl, alkylamino, carboalkoxy, carboxy,carboxamido, cyano, and Q^(b);

[0416] B is optionally selected from the group consisting of hydrido,trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8alkynyl, and C2-C8 haloalkyl, wherein each member of group B isoptionally substituted at any carbon up to and including 6 atoms fromthe point of attachment of B to A with one or more of the groupconsisting of R³², R³³, R³⁴, R³⁵, and R³⁶;

[0417] B is optionally a C3-C12 cycloalkyl or a C4-C9 saturatedheterocyclyl, wherein each ring carbon is optionally substituted withR³³, a ring carbon other than the ring carbon at the point of attachmentof B to A is optionally substituted with oxo provided that no more thanone ring carbon is substituted by oxo at the same time, ring carbons anda nitrogen adjacent to the carbon atom at the point of attachment areoptionally substituted with R⁹ or R¹³, a ring carbon or nitrogenadjacent to the R⁹ position and two atoms from the point of attachmentis optionally substituted with R¹⁰, a ring carbon or nitrogen adjacentto the R¹³ position and two atoms from the point of attachment isoptionally substituted with R¹², a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹⁰ position isoptionally substituted with R¹¹, a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹² position isoptionally substituted with R³³, and a ring carbon or nitrogen fouratoms from the point of attachment and adjacent to the R¹¹ and R³³positions is optionally substituted with R³⁴;

[0418] R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, alkoxyamino,alkanoyl, haloalkanoyl, amidino, guanidino, alkylenedioxy,haloalkylthio, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy,heteroaryloxy, heteroaralkoxy,heterocyclyloxy, heterocyclylalkoxy,hydroxy, amino, alkylamino, N-alkyl-N-arylamino, arylamino,aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino,heterocyclylalkylamino, alkylthio, alkylsulfinyl, arylsulfinyl,aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfamido,alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl,heteroarylsulfonyl, amidosulfonyl, alkyl, aryl, aralkyl, cycloalkyl,cycloalkylalkyl, heteroaryl, heterocyclyl, halo, haloalkyl, haloalkoxy,hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy,carboxyalkyl, carboxamido, and cyano;

[0419] A is a single covalent bond or (CH(R¹⁵))_(pa)—(W⁷)_(rr) whereinrr is 0 or 1, pa is an integer selected from 0 through 3, and W⁷ isselected from the group consisting of O, S, C(O), (R⁷)NC(O), (R⁷)NC(S),and N(R⁷);

[0420] R⁷ is selected from the group consisting of hydrido, hydroxy andalkyl;

[0421] R¹⁵ is selected from the group consisting of hydrido, hydroxy,halo, alkyl, and haloalkyl;

[0422] R¹ and X⁰ are independently selected from the group consisting ofhydrido, alkyl, cyano, halo, haloalkyl, haloalkoxy, amino, aminoalkyl,alkylamino, amidino, hydroxy, hydroxyamino, alkoxy, hydroxyalkyl,alkoxyamino, thiol, and alkylthio;

[0423] R² is Z⁰-Q;

[0424] Z⁰ is selected from the group consisting of covalent single bond,(CR⁴¹R⁴²)_(q) wherein q is 1 or 2, (CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p)wherein g and p are integers independently selected from 0 through 3 andW⁰ is selected from the group consisting of O, S, C(O), S(O), N(R⁴¹),and ON(R⁴¹);

[0425] Z⁰ is optionally (CH(R⁴¹))_(e)—W²²—(CH(R⁴²))_(h) wherein e and hare independently 0 or 1 and W²² is selected from the group consistingof CR⁴¹═CR⁴², 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl,1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl,2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl,1,2-piperazinyl, 1,3-piperazinyl, 2,3-piperazinyl, 2,6-piperazinyl,1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl,2,6-piperidinyl, 3,4-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl,2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl,2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, and3,4-tetrahydrofuranyl, wherein Z⁰ is directly bonded to the benzene ringand W²² is optionally substituted with one or more substituents selectedfrom the group consisting of R⁹, R¹⁰, R¹¹, R¹², and R¹³;

[0426] R⁴¹ and R⁴² are independently selected from the group consistingof hydrido, hydroxy, and amino;

[0427] Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein acarbon adjacent to the carbon at the point of attachment is optionallysubstituted by R⁹, the other carbon adjacent to the carbon at the pointof attachment is optionally substituted by R¹³, a carbon adjacent to R⁹and two atoms from the carbon at the point of attachment is optionallysubstituted by R¹⁰, a carbon adjacent to R¹³ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹², andany carbon adjacent to both R¹⁰ and R¹² is optionally substituted byR¹¹;

[0428] Q is optionally hydrido with the proviso that Z⁰ is other than acovalent single bond;

[0429] K is CHR^(4a) wherein R^(4a) is selected from the groupconsisting of hydrido, hydroxyalkyl, alkyl, alkoxyalkyl, alkylthioalkyl,and haloalkyl;

[0430] E⁰ is selected from the group consisting of a covalent singlebond, C(O)N(H), (H)NC(O), (R⁷)NS(O)₂, and S(O)₂N(R⁷);

[0431] Y^(AT), is Q^(b)-Q^(s);

[0432] Q^(s) is (CR³⁷R³⁸)_(b) wherein b is an integer selected from 1through 4, R³⁷ is selected from the group consisting of hydrido alkyland haloalkyl, and R³⁸ is selected from the group consisting of hydrido,alkyl, haloalkyl, aroyl, and heteroaroyl with the provisos that there isat least one aroyl or heteroaroyl substituent, that no more than onearoyl or heteroaroyl is bonded to (CR³⁷R³⁸)_(b) at the same time, thatsaid aroyl and said heteroaroyl are optionally substituted at from onethrough three of the ring carbons with a substituent selected from thegroup consisting of R¹⁶, R¹⁷, R¹⁸, and R¹⁹, that said aroyl and saidheteroaroyl are bonded to the CR³⁷R³⁸ that is directly bonded to E⁰,that no more than one alkyl or one haloalkyl is bonded to a CR³⁷R³⁸ atthe same time, and that said alkyl and haloalkyl are bonded to a carbonother than the one bonding said aroyl or said heteroaroyl;

[0433] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, haloalkylthio,alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio,alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo,haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

[0434] R¹⁶ or R¹⁹ is optionally selected from the group consisting ofNR²⁰R²¹, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the provisothat R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0435] Q^(b) is selected from the group consisting of NR²⁰R²¹, hydrido,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the provisos that nomore than one of R²⁰ and R²¹ is hydroxy, amino, alkylamino, ordialkylamino at the same time and that no more than one of R²³ and R²⁴is hydroxy, amino, alkylamino, or dialkylamino at the same time;

[0436] R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ are independently selected fromthe group consisting of hydrido, alkyl, hydroxy, amino, alkylamino anddialkylamino.

[0437] In a most preferred embodiment of a compound of Formula I, saidcompound is the Formula:

[0438] or a pharmaceutically acceptable salt thereof, wherein;

[0439] B is phenyl or a heteroaryl of 5 or 6 ring members, wherein acarbon adjacent to the carbon at the point of attachment of said phenylor heteroaryl ring to A is optionally substituted by R³², the othercarbon adjacent to the carbon at the point of attachment is optionallysubstituted by R³⁶, a carbon adjacent to R³² and two atoms from thecarbon at the point of attachment is optionally substituted by R³³, acarbon adjacent to R³⁶ and two atoms from the carbon at the point ofattachment is optionally substituted by R³⁵, and any carbon adjacent toboth R³³ and R³⁵ is optionally substituted by R³⁴;

[0440] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio,amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl,carboalkoxy, carboxy, carboxamido, cyano, and Q^(b);

[0441] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, haloalkylthio,alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl,alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl,haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

[0442] R¹⁶ or R¹⁹ is optionally NR²⁰R²¹ or C(NR²⁵)NR²³R²⁴ with theproviso that R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0443] Q^(b) is selected from the group consisting of NR²⁰R²¹, hydrido,and C(NR²⁵)NR²³R²⁴;

[0444] R²⁰, R²¹, R²³, R²⁴, and R²⁵ are independently hydrido or alkyl.

[0445] In another most preferred embodiment of a compound of Formula I,said compound is the Formula:

[0446] or a pharmaceutically acceptable salt thereof, wherein;

[0447] B is selected from the group consisting of hydrido, C2-C8 alkyl,C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each memberof group B is optionally substituted at any carbon up to and including 6atoms from the point of attachment of B to A with one or more of thegroup consisting of R³², R³³, R³⁴, R³⁵, and R³⁶;

[0448] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio,amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl,carboalkoxy, carboxy, carboxamido, cyano, and Q^(b);

[0449] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, haloalkylthio,alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl,alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl,haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

[0450] R¹⁶ or R¹⁹ is optionally selected from the group consisting ofNR²⁰R²¹, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the provisothat R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0451] Q^(b) is selected from the group consisting of NR²⁰R²¹, hydrido,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴;

[0452] R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ are independently hydrido oralkyl.

[0453] In still another most preferred embodiment of a compound ofFormula I, said compound is the Formula:

[0454] or a pharmaceutically acceptable salt thereof, wherein;

[0455] B is a C3-C7 cycloalkyl or a C4-C6 saturated heterocyclyl,wherein each ring carbon is optionally substituted with R³³, a ringcarbon other than the ring carbon at the point of attachment of B to Ais optionally substituted with oxo provided that no more than one ringcarbon is substituted by oxo at the same time, ring carbons and anitrogen adjacent to the carbon atom at the point of attachment areoptionally substituted with R⁹ or R¹³, a ring carbon or nitrogenadjacent to the R⁹ position and two atoms from the point of attachmentis optionally substituted with R¹⁰, a ring carbon or nitrogen adjacentto the R¹³ position and two atoms from the point of attachment isoptionally substituted with R¹², a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹⁰ position isoptionally substituted with R¹¹, a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹² position isoptionally substituted with R³³, and a ring carbon or nitrogen fouratoms from the point of attachment and adjacent to the R¹¹ and R³³positions is optionally substituted with R³⁴;

[0456] R³³ and R³⁴ are independently selected from the group consistingof hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy,hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl,alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy,carboxamido, and cyano;

[0457] R³³ is optionally Q^(b);

[0458] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, haloalkylthio,alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl,alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl,haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

[0459] R¹⁶ or R¹⁹ is optionally NR²⁰R²¹ or C(NR²⁵)NR²³R²⁴, with theproviso that R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0460] Q^(b) is selected from the group consisting of NR²⁰R²¹, hydrido,and C(NR²⁵)NR²³R²⁴;

[0461] R²⁰, R²¹, R²³, R²⁴, and R²⁵ are independently hydrido or alkyl.

[0462] The three groups of most preferred embodiment compounds of thepresent invention described above and having the Formula:

[0463] or a pharmaceutically acceptable salt thereof, have commonstructural units, wherein;

[0464] J is selected from the group consisting of halo, haloalkyl,hydroxy, hydroxyalkyl, amino, and aminoalkyl;

[0465] A is a single covalent bond or (CH(R¹⁵))_(pa)—(W⁷)_(rr) whereinrr is 0 or 1, pa is an integer selected from 0 through 3, and W⁷ isN(R⁷);

[0466] R⁷ is hydrido or alkyl;

[0467] R¹⁵ is selected from the group consisting of hydrido, halo,alkyl, and haloalkyl;

[0468] R¹ and X⁰ are independently selected from the group consisting ofhydrido, hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl,alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino,haloalkyl, haloalkoxy, and halo;

[0469] R² is Z⁰-Q;

[0470] Z⁰ is a covalent single bond;

[0471] Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein acarbon adjacent to the carbon at the point of attachment is optionallysubstituted by R⁹ the other carbon adjacent to the carbon at the pointof attachment is optionally substituted by R¹³, a carbon adjacent to R⁹and two atoms from the carbon at the point of attachment is optionallysubstituted by R¹⁰, a carbon adjacent to R¹³ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹², andany carbon adjacent to both R¹⁰ and R¹² is optionally substituted byR¹¹;

[0472] R⁹, R¹¹, and R¹³ are independently selected from the groupconsisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino,alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl,halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, andcyano;

[0473] R¹⁰ and R¹² are independently selected from the group consistingof hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy,alkoxyamino, hydroxy, amino, alkylamino, alkylsulfonamido,amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy,carboxy, carboxamido, carboxyalkyl, and cyano;

[0474] Y⁰ is phenyl or a heteroaryl of 5 or 6 ring members, wherein onecarbon of said phenyl or said heteroaryl is substituted by Q^(s), acarbon two or three contiguous atoms from the point of attachment ofQ^(s) is substituted by Q^(b), a carbon adjacent to the point ofattachment of Q^(s) is optionally substituted by R¹⁷, another carbonadjacent to the point of attachment of Q^(s) is optionally substitutedby R¹⁸, a carbon adjacent to Q^(b) is optionally substituted by R¹⁶, andanother carbon adjacent to Q^(b) is optionally substituted by R¹⁹;

[0475] Q^(s) is CH₂.

[0476] In another even more preferred specific embodiment of Formula I,compounds have the formula:

[0477] or a pharmaceutically acceptable salt thereof, wherein;

[0478] B is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl,5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl,2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl,4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to thecarbon at the point of attachment is optionally substituted by R³², theother carbon adjacent to the carbon at the point of attachment isoptionally substituted by R³⁶, a carbon adjacent to R³² and two atomsfrom the carbon at the point of attachment is optionally substituted byR³³, a carbon adjacent to R³⁶ and two atoms from the carbon at the pointof attachment is optionally substituted by R³⁵, and any carbon adjacentto both R³³ and R³⁵ is optionally substituted by R³⁴;

[0479] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, amidino, guanidino, carboxy, methoxy,ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino,acetamido, trifluoroacetamido, N-methylamino, dimethylamino,N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl,trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano,and Q^(b);

[0480] A is selected from the group consisting of single covalent bond,NH, N(CH₃), N(OH), CH₂, CH₃CH, CF₃CH, NHC(O), N(CH₃)C(O), C(O)NH,C(O)N(CH₃), CH₂CH₂, CH₂CH₂CH₂, CH₃CHCH₂, and CF₃CHCH₂;

[0481] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy,amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy,amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio,trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl,ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, and cyano;

[0482] R¹⁶ or R¹⁹ is optionally C(NR²⁵)NR²³R²⁴ with the proviso thatR¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0483] Q^(b) is C(NR²⁵)NR²³R²⁴ or hydrido, with the proviso that no morethan one of R²³ and R²⁴ is hydroxy at the same time;

[0484] R²³, R²⁴, and R²⁵ are independently selected from the groupconsisting of hydrido, methyl, ethyl, and hydroxy.

[0485] In still another even more preferred specific embodiment ofFormula I, compounds have the formula:

[0486] or a pharmaceutically acceptable salt thereof, wherein;

[0487] B is selected from the group consisting of hydrido, ethyl,2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butenyl, 3-butenyl,2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl,2-pentenyl, 3-pentenyl, 4-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl,1-methyl-2-butenyl, 1-methyl-3-butenyl, 1-methyl-2-butynyl, 3-pentyl,1-ethyl-2-propenyl, 2-methylbutyl, 2-methyl-2-butenyl,2-methyl-3-butenyl, 2-methyl-3-butynyl, 3-methylbutyl,3-methyl-2-butenyl, 3-methyl-3-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl,4-hexenyl, 5-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl,1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl,1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl,1-ethyl-3-butenyl, 1-propyl-2-propenyl, 1-ethyl-2-butynyl, 1-heptyl,2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 2-heptynyl,3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl,1-methyl-3-hexenyl, 1-methyl-4-hexenyl, 1-methyl-5-hexenyl,1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl,1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-4-pentenyl,1-butyl-2-propenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl,2,2,2-trifluoroethyl, 2,2-difluoropropyl,4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl,5,5,6,6,6-pentafluorohexyl, and 3,3,3-trifluoropropyl, wherein eachmember of group B is optionally substituted at any carbon up to andincluding 5 atoms from the point of attachment of B to A with one ormore of the group consisting of R³², R³³, R³⁴, R³⁵, and R³⁶;

[0488] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, amidino, guanidino, carboxy, methoxy,ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino,acetamido, trifluoroacetamido, N-methylamino, dimethylamino,N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl,trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano,and Q^(b);

[0489] A is selected from the group consisting of single covalent bond,NH, N(CH₃), N(OH), CH₂, CH₃CH, CF₃CH, NHC(O), N(CH₃)C(O), C(O)NH,C(O)N(CH₃), CH₂CH₂, CH₂CH₂CH₂, CH₃CHCH₂, and CF₃CHCH₂;

[0490] A is optionally selected from the group consisting of CH₂N(CH₃),CH₂N(CH₂CH₃), CH₂CH₂N(CH₃), and CH₂CH₂N(CH₂CH₃) with the proviso that Bis hydrido;

[0491] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy,amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy,amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio,trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl,ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, and cyano;

[0492] R¹⁶ or R¹⁹ is optionally selected from the group consisting ofNR²⁰R²¹, C(NR²⁵)NR²³R²⁴, and N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), with the provisothat R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0493] Q^(b) is selected from the group consisting of NR²⁰R²¹, hydrido,C(NR²⁵)NR²³R²⁴, and N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), with the provisos that nomore than one of R²⁰ and R²¹ is hydroxy at the same time and that nomore than one of R²³ and R²⁴ is hydroxy at the same time;

[0494] R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ are independently selected fromthe group consisting of hydrido, methyl, ethyl, propyl, butyl,isopropyl, and hydroxy.

[0495] In an additional even more preferred specific embodiment ofFormula I, compounds have the formula:

[0496] or a pharmaceutically acceptable salt thereof, wherein;

[0497] B is optionally selected from the group consisting ofcyclopropyl, cyclobutyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl,azetidin-3-yl, thiaetan-3-yl, cyclopentyl, cyclohexyl, norbomyl,7-oxabicyclo[2.2.1]heptan-2-yl, bicyclo[3.1.0]hexan-6-yl, cycloheptyl,2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl,2-piperazinyl, 1-piperidinyl, 2-piperidinyl, 3-piperidinyl,4-piperidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl,2-dioxanyl, 4H-2-pyranyl, 4H-3-pyranyl, 4H-4-pyranyl, 4H-pyranone-2-yl,4H-pyran-4-one-3-yl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl,2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl,2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein each ring carbonis optionally substituted with R³³, a ring carbon and nitrogen atomsadjacent to the carbon atom at the point of attachment is optionallysubstituted with R⁹ or R¹³, a ring carbon or nitrogen atom adjacent tothe R⁹ position and two atoms from the point of attachment is optionallysubstituted with R¹⁰, and a ring carbon or nitrogen atom adjacent to theR¹³ position and two atoms from the point of attachment is optionallysubstituted with R¹²;

[0498] A is selected from the group consisting of single covalent bond,NH, N(CH₃), N(OH), CH₂, CH₃CH, CF₃CH, NHC(O), N(CH₃)C(O), C(O)NH,C(O)N(CH₃), CH₂CH₂, CH₂CH₂CH₂, CH₃CHCH₂, and CF₃CHCH₂;

[0499] R³³ is selected from the group consisting of hydrido, amidino,guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy,amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido,N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio,isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, cyano, and Q^(b);

[0500] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy,amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy,amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio,trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl,ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, and cyano;

[0501] R¹⁶ or R¹⁹ is optionally C(NR²⁵)NR²³R²⁴ with the proviso thatR¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido;

[0502] Q^(b) is C(NR²⁵)NR²³R²⁴ or hydrido, with the proviso that no morethan one of R²³ and R²⁴ is hydroxy at the same time;

[0503] R²³, R²⁴, and R²⁵ are independently selected from the groupconsisting of hydrido, methyl, ethyl, and hydroxy.

[0504] The three groups of even more preferred specific embodimentcompounds of the present invention described herein and having theformula:

[0505] or a pharmaceutically acceptable salt thereof, have commonstructural units, wherein;

[0506] J is selected from the group consisting of fluoro, chloro,trifluoromethyl, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,1,2-dihydroxyethyl, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl,methoxy, trifluoromethoxy, N-methylamino, methythio, andtrifluoromethylthio;

[0507] R¹ and X⁰ are independently selected from the group consisting ofhydrido, hydroxy, amino, amidino, hydroxyamino, aminomethyl,1-aminoethyl, methylamino, dimethylamino, cyano, methyl, ethyl,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methoxyamino, methylthio,ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro,and bromo;

[0508] R² is Z⁰-Q;

[0509] Z is selected from the group consisting of covalent single bond,CH₂, CH₂CH₂, O, S, NH, N(CH₃), OCH₂, SCH₂, N(H)CH₂, and N(CH₃)CH₂;

[0510] Q is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl,5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl,2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl,4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to thecarbon at the point of attachment is optionally substituted by R⁹, theother carbon adjacent to the carbon at the point of attachment isoptionally substituted by R¹³, a carbon adjacent to R⁹ and two atomsfrom the carbon at the point of attachment is optionally substituted byR¹⁰, a carbon adjacent to R¹³ and two atoms from the carbon at the pointof attachment is optionally substituted by R¹², and any carbon adjacentto both R¹⁰ and R¹² is optionally substituted by R¹¹;

[0511] R⁹, R¹¹, and R¹³ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl,propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio,isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano;

[0512] R¹⁰ and R¹² are independently selected from the group consistingof hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl,propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl,1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino,methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl,N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl,2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl,ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl,N-(2-chlorobenzyl)anmidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl,N-(2-trifluoromethylbenzyl)amidocarbonyl,N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarhonyl,N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl,N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy,cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy,cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy,3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino,5-bromopyrid-2-yl-methylamino, 4-butoxyphenamino, 3-chlorobenzyl,4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino,4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy,4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl,5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy,2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy,3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy,2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy,3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy,3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy,3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy,4-fluorobenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy,3-fluoro-5-trifluoromethylbenzyloxy,4-fluoro-2-trifluoromethylbenzyloxy,4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy,2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy,4-fluorophenylamino, 2-fluorotrifluoromethylphenoxy,4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy,4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy,4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino,1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino,phenylsulfonyl, 3-trifluoromethoxybenzyloxy,4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy,4-trifluoromethoxyphenoxy, 3-trifluoromethylbenzyloxy,4-trifluoromethylbenzyloxy, 2,4-bis-trifluoromethylbenzyloxy,3-trifluoromethylbenzyl, 3,5-bis-trifluoromethylbenzyloxy,4-trifluoromethylphenoxy, 3-trifluoromethylphenoxy,3-trifluoromethylthiobenzyloxy, 4-trifluoromethylthiobenzyloxy,2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy,3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and3-trifluoromethylthiophenoxy;

[0513] Y⁰ is selected from the group of formulas consisting of:

[0514] Q^(s) is selected from the group consisting of a bond, CH₂, andCH₂CH₂.

[0515] In a most preferred specific embodiment of Formula I, compoundshave the formula;

[0516] or a pharmaceutically acceptable salt thereof, wherein;

[0517] B is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrol, 3-pyrrol, 2-imidazoyl,4-imidazoyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, and5-isoxazolyl, wherein a carbon adjacent to the carbon at the point ofattachment is optionally substituted by R³², the other carbon adjacentto the carbon at the point of attachment is optionally substituted byR³⁶, a carbon adjacent to R³² and two atoms from the carbon at the pointof attachment is optionally substituted by R³³, a carbon adjacent to R³⁶and two atoms from the carbon at the point of attachment is optionallysubstituted by R³⁵, and any carbon adjacent to both R³³ and R³⁵ isoptionally substituted by R³⁴;

[0518] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy,ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methoxyamino,methylthio, ethylthio, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, andQ^(b);

[0519] A is selected from the group consisting of single covalent bond,NH, N(CH₃), CH₂, CH₃CH, and CH₂CH₂;

[0520] Q^(b) is NR²⁰R²¹ or C(NR²⁵)NR²³R²⁴;

[0521] R²⁰, R²¹, R²³, R²⁴, and R²⁵ are independently selected from thegroup consisting of hydrido, methyl, and ethyl.

[0522] In another most preferred specific embodiment of Formula I,compounds have the formula:

[0523] or a pharmaceutically acceptable salt thereof, wherein;

[0524] B is selected from the group consisting of hydrido, ethyl,2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butenyl, 2-butynyl,sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl,3-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 3-pentyl, 2-methylbutyl,2-methyl-2-butenyl, 3-methylbutyl, 3-methyl-2-butenyl, 1-hexyl,2-hexenyl, 3-hexenyl, 4-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl,2-hexyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-2-pentynyl,1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-heptyl, 2-heptenyl,3-heptenyl, 4-heptenyl, 5-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl,5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl,1-methylhexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl,1-methyl-4-hexynyl, 3-heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl,1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl,2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl,4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and3,3,3-trifluoropropyl, wherein each member of group B is optionallysubstituted at any carbon up to and including 5 atoms from the point ofattachment of B to A with one or more of the group consisting of R³²,R³³, R³⁴, R³⁵, and R³⁶;

[0525] R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy,ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methoxyamino,methylthio, ethylthio, trifluoromethyl, pentafluoroethyl,2,2,2-tifluoroethyl, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, andQ^(b);

[0526] A is selected from the group consisting of single covalent bond,NH, N(CH₃), CH₂, CH₃CH, and CH₂CH₂;

[0527] A is optionally selected from the group consisting of CH₂N(CH₃),CH₂N(CH₂CH₃), CH₂CH₂N(CH₃), and CH₂CH₂N(CH₂CH₃) with the proviso that Bis hydrido;

[0528] Q^(b) is selected from the group consisting of NR²⁰R²¹,C(NR²⁵)NR²³R²⁴, and N(R²⁶)C(NR^(25)N(R) ²³)(R²⁴);

[0529] R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ are independently selected fromthe group consisting of hydrido, methyl, and ethyl.

[0530] In still another most preferred specific embodiment of Formula I,compounds have the formula:

[0531] or a pharmaceutically acceptable salt thereof, wherein;

[0532] B is selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, oxalan-2-yl,2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl,azetidin-3-yl, bicyclo[3.1.0]hexan-6-yl, 2-morpholinyl, 3-morpholinyl,4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl,2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl,2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl, 2-tetrahydrofuranyl,3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl,4-tetrahydropyranyl, 2-tetrahydrothienyl, and 3-tetrahydrothienyl,wherein each ring carbon is optionally substituted with R³³, ringcarbons and a nitrogen adjacent to the carbon atom at the point ofattachment are optionally substituted with R⁹ or R¹³, a ring carbon ornitrogen adjacent to the R⁹ position and two atoms from the point ofattachment are optionally substituted with R¹⁰, and a ring carbon ornitrogen atom adjacent to the R¹³ position and two atoms from the pointof attachment is optionally substituted with R¹²;

[0533] R³³ is selected from the group consisting of hydrido, amidino,guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, carboxy, amino,N-methylamino, dimethylamino, methoxyamino, methylthio, ethylthio,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro,bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl,amidocarbonyl, cyano, and Q^(b);

[0534] A is selected from the group consisting of single covalent bond,NH, N(CH₃), CH₂, CH₃CH, and CH₂CH₂;

[0535] Q^(b) is NR²⁰R²¹ or C(NR²⁵)NR²³R²⁴;

[0536] R²⁰, R²¹, R²³, R²⁴, and R²⁵ are independently selected from thegroup consisting of hydrido, methyl, and ethyl.

[0537] The three groups of the most preferred specific embodimentcompounds of the present invention having the formula:

[0538] or a pharmaceutically acceptable salt thereof, have commonstructural units, wherein;

[0539] J is selected from the group consisting of fluoro, chloro,trifluoromethyl, hydroxy, hydroxymethyl, amino, and aminomethyl;

[0540] X⁰ is selected from the group consisting of hydrido, hydroxy,amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl,hydroxymethyl, chloro, and fluoro;

[0541] R¹ is selected from the group consisting of hydrido, hydroxy,hydroxymethyl, amino, aminomethyl, methylamino, cyano, methyl,trifluoromethyl, methoxy, methylthio, trifluoromethoxy, fluoro, andchloro;

[0542] R² is selected from the group consisting of phenyl, 2-thienyl,2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl,and 3-pyridyl, wherein a carbon adjacent to the carbon at the point ofattachment is optionally substituted by R⁹, the other carbon adjacent tothe carbon at the point of attachment is optionally substituted by R¹³,a carbon adjacent to R⁹ and two atoms from the carbon at the point ofattachment is optionally substituted by R¹⁰, a carbon adjacent to R¹³and two atoms from the carbon at the point of attachment is optionallysubstituted by R¹², and any carbon adjacent to both R¹⁰ and R¹² isoptionally substituted by R¹¹;

[0543] R⁹, R¹¹, and R¹³ are independently selected from the groupconsisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino,N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl,carboxy, and cyano;

[0544] R¹⁰ and R¹² are independently selected from the group consistingof hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl,N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,N-(3-fluorobenzyl)amidocarbonyl,N-(2-trifluoromethylbenzyl)amidocarbonyl,N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl,N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl,N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy,hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy,carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino,dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl,N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro,chloro, bromo, and cyano;

[0545] Y⁰ is selected from the group of formulas consisting of:

[0546] R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy,hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,dimethylamino, methylthio, ethylthio, trifluoromethylthio,methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl,2,2,2-trfluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl,carboxy, and cyano;

[0547] Q^(s) is CH₂.

[0548] The compounds of this invention can be used in anticoagulanttherapy for the treatment and prevention of a variety of thromboticconditions including coronary artery and cerebrovascular disease. Thecompounds of this invention can be used to inhibit serine proteaseassociated with the coagulation cascade and factors II, VII, VIII, IX,X, XI, or XII. The compounds of the invention can inhibit the formationof blood platelet aggregates, inhibit the formation of fibrin, inhibitthrombus formation, and inhibiting embolus formation in a mammal, inblood, in blood products, and in mammalian organs. The compounds alsocan be used for treating or preventing unstable angina, refractoryangina, myocardial infarction, transient ischemic attacks, atrialfibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis,disseminated intravascular coagulation, ocular build up of fibrin, andreocclusion or restenosis of recanalized vessels in a mammal. Thecompounds can also be used in prophylactic treatment of subjects who areat risk of developing such disorders. The compounds can be used to lowerthe risk of atherosclerosis. The compounds of Formula (1) would also beuseful in prevention of cerebral vascular accident (CVA) or stroke.

[0549] Besides being useful for human treatment, these compounds arealso useful for veterinary treatment of companion animals, exoticanimals and farm animals, including mammals, rodents, and the like. Morepreferred animals include horses, dogs, and cats.

[0550] In yet another embodiment of the present invention, the novelcompounds are selected from the compounds set forth in the Examples,Table 1, and in the General Synthetic Procedures and Specific Examplessection.

[0551] The use of generic terms in the description of the compounds areherein defined for clarity.

[0552] Standard single letter elemental symbols are used to representspecific types of atoms unless otherwise defined. The symbol “C”represents a carbon atom. The symbol “O” represents an oxygen atom. Thesymbol “N” represents a nitrogen atom. The symbol “P” represents aphosphorus atom. The symbol “S” represents a sulfur atom. The symbol “H”represents a hydrido atom. Double letter elemental symbols are used asdefined for the elements of the periodical table (i.e, Cl representschlorine, Se represents selenium, etc.).

[0553] As utilized herein, the term “alkyl”, either alone or withinother terms such as “haloalkyl” and “alkylthio”, means an acyclic alkylradical containing from 1 to about 10, preferably from 3 to about 8carbon atoms and more preferably 3 to about 6 carbon atoms. Said alkylradicals may be optionally substituted with groups as defined below.Examples of such radicals include methyl, ethyl, chloroethyl,hydroxyethyl, n-propyl, oxopropyl, isopropyl, n-butyl, cyanobutyl,isobutyl, sec-butyl, tert-butyl, pentyl, aminopentyl, iso-amyl, hexyl,octyl and the like.

[0554] The term “alkenyl” refers to an unsaturated, acyclic hydrocarbonradical in so much as it contains at least one double bond. Such alkenylradicals contain from about 2 to about 10 carbon atoms, preferably fromabout 3 to about 8 carbon atoms and more preferably 3 to about 6 carbonatoms. Said alkenyl radicals may be optionally substituted with groupsas defined below. Examples of suitable alkenyl radicals includepropenyl, 2-chloropropenyl, buten-1-yl, isobutenyl, penten-1-yl,2-2-methylbuten-1-yl, 3-methylbuten-1-yl, hexen-1-yl,3-hydroxyhexen-1-yl, hepten-1-yl, and octen-1-yl, and the like.

[0555] The term “alkynyl” refers to an unsaturated, acyclic hydrocarbonradical in so much as it contains one or more triple bonds, suchradicals containing about 2 to about 10 carbon atoms, preferably havingfrom about 3 to about 8 carbon atoms and more preferably having 3 toabout 6 carbon atoms. Said alkynyl radicals may be optionallysubstituted with groups as defined below. Examples of suitable alkynylradicals include ethynyl, propynyl, hydroxypropynyl, butyn-1-yl,butyn-2-yl, pentyn-1-yl, pentyn-2-yl, 4-methoxypentyn-2-yl,3-methylbutyn-1-yl, hexyn-1-yl, hexyn-2-yl, hexyn-3-yl,3,3-dimethylbutyn-1-yl radicals and the like.

[0556] The term “hydrido” denotes a single hydrogen atom (H). Thishydrido radical may be attached, for example, to an oxygen atom to forma “hydroxyl” radical, one hydrido radical may be attached to a carbonatom to form a “methine” radical —CH═, or two hydrido radicals may beattached to a carbon atom to form a “methylene” (—CH₂—) radical.

[0557] The term “carbon” radical denotes a carbon atom without anycovalent bonds and capable of forming four covalent bonds.

[0558] The term “cyano” radical denotes a carbon radical having three offour covalent bonds shared by a nitrogen atom.

[0559] The term “hydroxyalkyl” embraces radicals wherein any one or moreof the alkyl carbon atoms is substituted with a hydroxyl as definedabove. Specifically embraced are monohydroxyalkyl, dihydroxyalkyl andpolyhydroxyalkyl radicals.

[0560] The term “alkanoyl” embraces radicals wherein one or more of theterminal alkyl carbon atoms are substituted with one or more carbonylradicals as defined below. Specifically embraced are monocarbonylalkyland dicarbonylalkyl radicals. Examples of monocarbonylalkyl radicalsinclude formyl, acetyl, and pentanoyl. Examples of dicarbonylalkylradicals include oxalyl, malonyl, and succinyl.

[0561] The term “alkylene” radical denotes linear or branched radicalshaving from 1 to about 10 carbon atoms and having attachment points fortwo or more covalent bonds. Examples of such radicals are methylene,ethylene, methylethylene, and isopropylidene.

[0562] The term “alkenylene” radical denotes linear or branched radicalshaving from 2 to about 10 carbon atoms, at least one double bond, andhaving attachment points for two or more covalent bonds. Examples ofsuch radicals are 1,1-vinylidene (CH₂═C), 1,2-vinylidene (—CH═CH—), and1,4-butadienyl (—CH═CH—CH═CH—).

[0563] The term “halo” means halogens such as fluorine, chlorine,bromine or iodine atoms.

[0564] The term “haloalkyl” embraces radicals wherein any one or more ofthe alkyl carbon atoms is substituted with halo as defined above.Specifically embraced are monohaloalkyl, dihaloalkyl and polyhaloalkylradicals. A monohaloalkyl radical, for one example, may have either abromo, chloro or a fluoro atom within the radical. Dihalo radicals mayhave two or more of the same halo atoms or a combination of differenthalo radicals and polyhaloalkyl radicals may have more than two of thesame halo atoms or a combination of different halo radicals. Morepreferred haloalkyl radicals are “haloalkyl” radicals having one toabout six carbon atoms. Examples of such haloalkyl radicals includefluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl,dichloromethyl, trichloromethyl, trifluoroethyl, pentafluoroethyl,heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl,difluoroethyl, difluoropropyl, dichloroethyl and dichloropropyl.

[0565] The term “hydroxyhaloalkyl” embraces radicals wherein any one ormore of the haloalkyl carbon atoms is substituted with hydroxy asdefined above Examples of “hydroxyhaloalkyl” radicals includebexafluorohydroxypropyl.

[0566] The term “haloalkylene radical” denotes alkylene radicals whereinany one or more of the alkylene carbon atoms is substituted with halo asdefined above. Dihalo alkylene radicals may have two or more of the samehalo atoms or a combination of different halo radicals andpolyhaloalkylene radicals may have more than two of the same halo atomsor a combination of different halo radicals. More preferred haloalkyleneradicals are “haloalkylene” radicals having one to about six carbonatoms. Examples of “haloalkylene” radicals include difluoromethylene,tetrafluoroethylene, tetrachloroethylene, alkyl substitutedmonofluoromethylene, and aryl substituted trifluoromethylene.

[0567] The term “haloalkenyl” denotes linear or branched radicals havingfrom 1 to about 10 carbon atoms and having one or more double bondswherein any one or more of the alkenyl carbon atoms is substituted withhalo as defined above. Dihaloalkenyl radicals may have two or more ofthe same halo atoms or a combination of different halo radicals andpolyhaloalkenyl radicals may have more than two of the same halo atomsor a combination of different halo radicals.

[0568] The terms “alkoxy” and “alkoxyalkyl” embrace linear or branchedoxy-containing radicals each having alkyl portions of one to about tencarbon atoms, such as methoxy radical. The term “alkoxyalkyl” alsoembraces alkyl radicals having one or more alkoxy radicals attached tothe alkyl radical, that is, to form monoalkoxyalkyl and dialkoxyalkylradicals. More preferred alkoxy radicals are “alkoxy” radicals havingone to six carbon atoms. Examples of such radicals include methoxy,ethoxy, propoxy, butoxy, isopropoxy and tert-butoxy alkyls. The “alkoxy”radicals may be further substituted with one or more halo atoms, such asfluoro, chloro or bromo, to provide “haloalkoxy” and “haloalkoxyalkyl”radicals. Examples of such haloalkoxy radicals include fluoromethoxy,chloromethoxy, trifluoromethoxy, difluoromethoxy, trifluoroethoxy,fluoroethoxy, tetrafluoroethoxy, pentafluoroethoxy, and fluoropropoxy.Examples of such haloalkoxyalkyl radicals include fluoromethoxymethyl,chloromethoxyethyl, trifuoromethoxymethyl, difluoromethoxyethyl, andtrifluoroethoxynethyl.

[0569] The terms “alkenyloxy” and “alkenyloxyalkyl” embrace linear orbranched oxy-containing radicals each having alkenyl portions of two toabout ten carbon atoms, such as ethenyloxy or propenyloxy radical Theterm “alkenyloxyalkyl” also embraces alkenyl radicals having one or morealkenyloxy radicals attached to the alkyl radical, that is, to formmonoalkenyloxyalkyl and dialkenyloxyalkyl radicals. More preferredalkenyloxy radicals are “alkenyloxy” radicals having two to six carbonatoms. Examples of such radicals include ethenyloxy, propenyloxy,butenyloxy, and isopropenyloxy alkyls. The “alkenyloxy” radicals may befurther substituted with one or more halo atoms, such as fluoro, chloroor bromo, to provide “haloalkenyloxy” radicals. Examples of suchradicals include trifluoroethenyloxy, fluoroethenyloxy,difluoroethenyhloxy, and fluoropropenyloxy.

[0570] The term “haloalkoxyalkyl” also embraces alkyl radicals havingone or more haloalkoxy radicals attached to the alkyl radical, that is,to form monohaloalkoxyalkyl and dihaloalkoxyalkyl radicals. The term“haloalkenyloxy” also embraces oxygen radicals having one or morehaloalkenyloxy radicals attached to the oxygen radical, that is, to formmonohaloalkenyloxy and dihaloalkenyloxy radicals. The term“haloalkenyloxyalkyl” also embraces alkyl radicals having one or morehaloalkenyloxy radicals attached to the alkyl radical, that is, to formmonohaloalkenyloxyalkyl and dihaloalkenyloxyalkyl radicals.

[0571] The term “allkylenedioxy” radicals denotes alkylene radicalshaving at least two oxygens bonded to a single alkylene group. Examplesof “alkylenedioxy” radicals include methylenedioxy, ethylenedioxy,alkylsubstituted methylenedioxy, and arylsubstituted methylenedioxy. Theterm “haloalkylenedioxy” radicals denotes haloalkylene radicals havingat least two oxy groups bonded to a single haloalkyl group. Examples of“haloalkylenedioxy” radicals include difluoromethylenedioxy,tetrafluoroethylenedioxy, tetrachloroethylenedioxy, alkylsubstitutedmonofluoromethylenedioxy, and arylsubstituted monofluoromethylenedioxy.

[0572] The term “aryl”, alone or in combination, means a carbocyclicaromatic system containing one, two or three rings wherein such ringsmay be attached together in a pendant manner or may be fused. The term“fused” means that a second ring is present (ie, attached or formed) byhaving two adjacent atoms in common (ie, shared) with the first ring.The term “fused” is equivalent to the term “condensed”. The term “aryl”embraces aromatic radicals such as phenyl, naphthyl, tetrahydronaphthyl,indane and biphenyl.

[0573] The term “perhaloaryl” embraces aromatic radicals such as phenyl,naphthyl, tetrahydronaphthyl, indane and biphenyl wherein the arylradical is substituted with 3 or more halo radicals as defined below.

[0574] The term “heterocyclyl” embraces saturated and partiallysaturated heteroatom-containing ring-shaped radicals having from 4through 15 ring members, herein referred to as “C4-C15 heterocyclyl”,selected from carbon, nitrogen, sulfur and oxygen, wherein at least onering atom is a heteroatom. Heterocyclyl radicals may contain one, two orthree rings wherein such rings may be attached in a pendant manner ormay be fused. Examples of saturated heterocyclic radicals includesaturated 3 to 6-membered heteromonocylic group containing 1 to 4nitrogen atoms[e.g. pyrrolidinyl, imidazolidinyl, piperidino,piperazinyl, etc.]; saturated 3 to 6-membered heteromonocyclic groupcontaining 1 to 2 oxygen atoms and 1 to 3 nitrogen atoms [e.g.morpholinyl, etc.]; saturated 3 to 6-membered heteromonocyclic groupcontaining, 1 to 2 sulfur atoms and 1 to 3 nitrogen atoms [e.g.,thiazolidinyl, etc.]. Examples of partially saturated heterocyclylradicals include dihydrothiophene, dihydropyran, dihydrofuran anddihydrothiazole. Non-limiting examples of heterocyclic radicals include2-pyrrolinyl, 3-pyrrolinyl, pyrrolindinyl, 1,3-dioxolanyl, 2H-pyranyl,4H-pyranyl, piperidinyl, 1,4-dioxanyl, morpholinyl, 1,4-dithianyl,thiomorpholinyl, and the like. Said “heterocyclyl” group may besubstituted as defined herein. Preferred heterocyclic radicals includefive to twelve membered fused or unfused radicals.

[0575] The term “heteroaryl” embraces fully unsaturatedheteroatom-containing ring-shaped aromatic radicals having from 4through 15 ring members selected from carbon, nitrogen, sulfur andoxygen, wherein at least one ring atom is a heteroatom. Heteroarylradicals may contain one, two or three rings wherein such rings may beattached in a pendant manner or may be fused. Examples of “heteroaryl”radicals, include the unsaturated heteromonocyclyl group of 5 to 6contiguous members containing 1 to 4 nitrogen atoms, for example,pyrrolyl, pyrrolinyl, imidazolyl, pyrazolyl, 2-pyridyl, 3-pyridyl,4-pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazolyl [e.g.,4H-1,2,4-triazolyl, 1H-1,2,3-triazolyl, 2H-1,2,3-triazolyl, etc.]tetrazolyl [e.g. 1H-tetrazolyl, 2H-tetrazolyl, etc.], etc.; unsaturatedcondensed heterocyclic group containing 1 to 5 nitrogen atoms, forexample, indolyl, isoindolyl, indolizinyl, benziidazolyl, quinolyl,isoquinolyl, indazolyl, benzotriazolyl, tetrazolopyridazinyl [e.g.,tetrazolo [1,5-b]pyridazinyl, etc.], etc.; unsaturated 3 to 6-memberedheteromonocyclic group containing an oxygen atom, for example, pyranyl,2-furyl, 3-furyl, etc.; unsaturated 5 to 6-membered heteromonocyclicgroup containing a sulfur atom, for example, 2-thienyl, 3-thienyl, etc.;unsaturated 5- to 6-membered heteromonocyclic group containing 1 to 2oxygen atoms and 1 to 3 nitrogen atoms, for example, oxazolyl,isoxazolyl, oxadiazolyl [e.g., 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl,1,2,5-oxadiazolyl, etc.] etc.; unsaturated condensed heterocyclic groupcontaining 1 to 2 oxygen atoms and 1 to 3 nitrogen atoms [e.g.benzoxazolyl, benzoxadiazolyl, etc.]; unsaturated 5 to 6-memberedheteromonocyclic group containing 1 to 2 sulfur atoms and 1 to 3nitrogen atoms, for example, thiazolyl, thiadiazolyl [e.g.,1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,5-thiadiazolyl, etc.]etc.;unsaturated condensed heterocyclic group containing 1 to 2 sulfur atomsand 1 to 3 nitrogen atoms [e.g., benzothiazolyl, benzothiadiazolyl,etc.] and the like. The term also embraces radicals where heterocyclicradicals are fused with aryl radicals. Examples of such fused bicyclicradicals include benzofuran, benzothiophene, and the like. Said“heteroaryl” group may be substituted as defined herein. Preferredheteroaryl radicals include five and six membered unfused radicals.Non-limiting examples of heteroaryl radicals include 2-thienyl,3-thienyl, 2-furyl, 3-foryl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 1,2,4-triazol-3-yl,1,2,4-triazol-5-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl,1,3,4-oxadiazol-3-yl, 1,3,4-oxadiazol-5-yl, 3-isothiazolyl,5-isothiazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl,2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl,4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl,1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl,1,2,4-triazin-6-yl, 1,2,3-triazinyl, and 1,2,3-triazin-5-yl, and thelike.

[0576] The term “sulfonyl”, whether used alone or linked to other termssuch as alkylsulfonyl, denotes respectively divalent radicals —SO₂ 13 .“Alkylsulfonyl”, embraces alkyl radicals attached to a sulfonyl radical,where alkyl is defined as above. “Alkylsulfonylalkyl”, embracesalkylsulfonyl radicals attached to an alkyl radical, where alkyl isdefined as above. “Haloalkylsulfonyl”, embraces haloalkyl radicalsattached to a sulfonyl radical, where haloalkyl is defined as above.“Haloalkylsulfonylalkyl”, embraces haloalkylsulfonyl radicals attachedto an alkyl radical, where alkyl is defined as above.

[0577] The term “amidosulfonyl” embraces amino, monoalkylamino,dialkylamino, monocycloalkylamino, alkyl cycloalkylamino,dicycloalkylamino, N-alkyl-N-arylamino, arylamino, aralkylamino,nitrogen containing heterocyclyl, heterocyclylamino,N-alkyl-N-heterocyclylamino, heteroarylamino, and heteroaralkylaminoradicals, attached to one of two unshared bonds in a sulfonyl radical.

[0578] The term “sulfinyl”, whether used alone or linked to other termssuch as alkylsulfinyl, denotes respectively divalent radicals —S(O)—.“Alkylsulfinyl”, embraces alkyl radicals attached to a sulfinyl radical,where alkyl is defined as above. “Alkylsulfinylalkyl”, embracesalkylsulfinyl radicals attached to an alkyl radical, where alkyl isdefined as above. “Haloalkylsulfinyl”, embraces haloalkyl radicalsattached to a sulfinyl radical, where haloalkyl is defined as above.“Haloalkylsulfinylalkyl”, embraces haloalkylsulfinyl radicals attachedto an alkyl radical, where alkyl is defined as above.

[0579] The term “aralkyl” embraces aryl-substituted alkyl radicals.Preferable aralkyl radicals are “aralkyl” radicals having aryl radicalsattached to alkyl radicals having one to six carbon atoms. Examples ofsuch radicals include benzyl, diphenylmethyl, triphenylmethyl,phenylethyl and diphenylethyl. The terms benzyl and phenylmethyl areinterchangeable.

[0580] The term “heteroaralkyl” embraces heteroaryl-substituted alkylradicals wherein the heteroaralkyl radical may be additionallysubstituted with three or more substituents as defined above for aralkylradicals. The term “perhaloaralkyl” embraces aryl-substituted alkylradicals wherein the aralkyl radical is substituted with three or morehalo radicals as defined above.

[0581] The term “aralkylsulfinyl”, embraces aralkyl radicals attached toa sulfinyl radical, where aralkyl is defined as above.“Aralkylsulfonylalkyl”, embraces aralkylsulfinyl radicals attached to analkyl radical, where alkyl is defined as above.

[0582] The term “aralkylsulfonyl”, embraces aralkyl radicals attached toa sulfonyl radical, where aralkyl is defined as above.“Aralkylsulfonylalkyl”, embraces aralkylsulfonyl radicals attached to analkyl radical, where alkyl is defined as above.

[0583] The term “cycloalkyl” embraces radicals having three to 15 carbonatoms. More preferred cycloalkyl radicals are “cycloalkyl” radicalshaving three to seven carbon atoms. Examples include radicals such ascyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl. Theterm cycloalkyl embraces radicals having seven to 15 carbon atoms andhaving two to four rings. Examples include radicals such as norbornyl(i.e., bicyclo[2.2.1]heptyl) and adamantyl. The term “cycloalkylalkyl”embraces cycloalkyl-substituted alkyl radicals. Preferablecycloalkylalkyl radicals are “cycloalkylalky” radicals having cycloalkylradicals attached to alkyl radicals having one to six carbon atoms.Examples of such radicals include cyclobexylhexyl. The term“cycloalkenyl” embraces radicals having three to ten carbon atoms andone or more carbon-carbon double bonds. Preferred cycloalkenyl radicalsare “cycloalkenyl” radicals having three to seven carbon atoms. Examplesinclude radicals such as cyclobutenyl, cyclopentenyl, cyclohexenyl andcycloheptenyl. The term “halocycloalkyl” embraces radicals wherein anyone or more of the cycloalkyl carbon atoms is substituted with halo asdefined above. Specifically embraced are monohalocycloalkyl,dihalocycloalkyl and polyhalocycloalkyl radicals. A monohalocycloalkylradical, for one example, may have either a bromo, chloro or a fluoroatom within the radical. Dihalo radicals may have two or more of thesame halo atoms or a combination of different halo radicals andpolyhalocycloalkyl radicals may have more than two of the same haloatoms or a combination of different halo radicals. More preferredhalocycloalkyl radicals are “halocycloalkyl” radicals having three toabout eight carbon atoms. Examples of such halocycloalkyl radicalsinclude fluorocyclopropyl, difluorocyclobutyl, trifluorocyclopentyl,tetrafluorocyclohexyl, and dichlorocyclopropyl. The term“halocycloalkenyl” embraces radicals wherein any one or more of thecycloalkenyl carbon atoms is substituted with halo as defined above.Specifically embraced are monohalocycloalkenyl, dihalocycloalkenyl andpolyhalocycloalkenyl radicals.

[0584] The term “cycloalkoxy” embraces cycloalkyl radicals attached toan oxy radical. Examples of such radicals includes cyclohexoxy andcyclopentoxy. The term “cycloalkoxyalkyl” also embraces alkyl radicalshaving one or more cycloalkoxy radicals attached to the alkyl radical,that is, to form monocycloalkoxyalkyl and dicycloalkoxyalkyl radicals.Examples of such radicals include cyclohexoxyethyl. The “cycloalkoxy”radicals may be further substituted with one or more halo atoms, such asfluoro, chloro or bromo, to provide “halocycloalkoxy” and“halocycloalkoxyalkyl” radicals.

[0585] The term “cycloalkylalkoxy” embraces cycloalkyl radicals attachedto an alkoxy radical. Examples of such radicals includescyclohexylmethoxy and cyclopentylmethoxy.

[0586] The term “cycloalkenyloxy” embraces cycloalkenyl radicalsattached to an oxy radical. Examples of such radicals includescyclohexenyloxy and cyclopentenyloxy. The term “cycloalkenyloxyalkyl”also embraces alkyl radicals having one or more cycloalkenyloxy radicalsattached to the alkyl radical, that is, to form monocycloalkenyloxyalkyland dicycloalkenyloxyalkyl radicals. Examples of such radicals includecyclohexenyloxyethyl. The “cycloalkenyloxy” radicals may be furthersubstituted with one or more halo atoms, such as fluoro, chloro orbromo, to provide “halocycloalkenyloxy” and “halocycloalkenyloxyalkyl”radicals.

[0587] The term “cycloalkylenedioxy” radicals denotes cycloalkyleneradicals having at least two oxygens bonded to a single cycloalkylenegroup. Examples of “alkylenedioxy” radicals include1,2-dioxycyclohexylene.

[0588] The term “cycloalkylsulfinyl”, embraces cycloalkyl radicalsattached to a sulfinyl radical, where cycloalkyl is defined as above.“Cycloalkylsulfinylalkyl”, embraces cycloalkylsulfinyl radicals attachedto an alkyl radical, where alkyl is defined as above. The term“Cycloalkylsulfonyl”, embraces cycloalkyl radicals attached to asulfonyl radical, where cycloalkyl is defined as above.“Cycloalkylsulfonylalkyl”, embraces cycloalkylsulfonyl radicals attachedto an alkyl radical, where alkyl is defined as above.

[0589] The term “cycloalkylalkanoyl” embraces radicals wherein one ormore of the cycloalkyl carbon atoms are substituted with one or morecarbonyl radicals as defined below. Specifically embraced aremonocarbonylcycloalkyl and dicarbonylcycloalkyl radicals. Examples ofmonocarbonylcycloalkyl radicals include cyclohexylcarbonyl,cyclohexylacetyl, and cyclopentylcarbony!. Examples ofdicarbonylcycloalkyl radicals include 1,2-dicarbonylcyclohexane.

[0590] The term “alkylthio” embraces radicals containing a linear orbranched alkyl radical, of one to ten carbon atoms, attached to adivalent sulfur atom. More preferred alkylthio radicals are “alkylthio”radicals having one to six carbon atoms. An example of “alkylthio” ismethylthio (CH₃—S—). The “alkylthio” radicals may be further substitutedwith one or more halo atoms, such as fluoro, chloro or bromo, to provide“haloalkylthio” radicals. Examples of such radicals includefluoromethylthio, chloromethylthio, trifluoromethylthio,difluorometbylthio, trifluoroethylthio, fluoroethylthio,tetrafluoroethylthio, pentafluoroethylthio, and fluoropropylthio.

[0591] The term “alkyl aryl amino” embraces radicals containing a linearor branched alkyl radical, of one to ten carbon atoms, and one arylradical both attached to an amino radical. Examples include N-methylmethoxyaniline, N-ethyl-4-methoxyaniline, andN-methylktrifluoromethoxyaniline.

[0592] The term alkylamino denotes “monoalkylamino” and “dialkylamino”containing one or two alkyl radicals, respectively, attached to an aminoradical. One or two alkyl radicals of the alkylamino may be optionallysubstituted with hydrogen bonding substitutents selected from the groupconsisting of hydroxy, amino, monoalkylamino, dialkylamino, amidino,guanidino, thiol, and alkoxy provided the alkyl radicals comprises twoor more carbons.

[0593] The terms arylamino denotes “monoarylamino” and “diarylamino”containing one or two aryl radicals, respectively, attached to an aminoradical. Examples of such radicals include N-phenylamino andN-naphthylamino.

[0594] The term “aralkylamino”, embraces aralkyl radicals attached to anamino radical, where aralkyl is defined as above. The term aralkylaminodenotes “monoaralkylamino” and “diaralkylamino.” containing one or twoaralkyl radicals, respectively, attached to an amino radical. The termaralkylamino further denotes “monoaralkyl monoalkylamino” containing onearalkyl radical and one alkyl radical attached to an amino radical.

[0595] The term “arylsulfinyl” embraces radicals containing an arylradical, as defined above, attached to a divalent S(O) atom. The term“arylsulfinylalkyl” denotes arylsulfinyl radicals attached to a linearor branched alkyl radical, of one to ten carbon atoms.

[0596] The term “arylsulfonyl”, embraces aryl radicals attached to asulfonyl radical, where aryl is defined as above. “arylsulfonylalkyl”,embraces arylsulfonyl radicals attached to an alkyl radical, where alkylis defined as above. The term “heteroarylsulfinyl” embraces radicalscontaining an heteroaryl radical, as defined above, attached to adivalent S(O) atom. The term “heteroarylsulfinylalkyl” denotesheteroarylsulfinyl radicals attached to a linear or branched alkylradical, of one to ten carbon atoms. The term “Heteroarylsulfonyl”,embraces heteroaryl radicals attached to a sulfonyl radical, whereheteroaryl is defined as above. “Heteroarylsulfonylalkyl”, embracesheteroarylsulfonyl radicals attached to an alkyl radical, where alkyl isdefined as above.

[0597] The term “aryloxy” embraces aryl radicals, as defined above,attached to an oxygen atom. Examples of such radicals include phenoxy,4-chloro-3-ethylphenoxy, 4-chloro-3-methylphenoxy,3-chloro-4-ethylphenoxy, 3,4-dichlorophenoxy, 4-methylphenoxy,3-trifluoromethoxyphenoxy, 3-trifluoromethylphenoxy, 4-fluorophenoxy,3,4-dimethylphenoxy, 5-bromo-2-fluorophenoxy, 4-bromo-3-fluorophenoxy,4-fluoro-3-methylphenoxy, 5,6,7,8-tetrahydronaphthyloxy,3-isopropylphenoxy, 3-cyclopropylphenoxy, 3-ethylphenoxy,3-pentafluoroethyiphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)-phenoxy, and4-tert -butylphenoxy.

[0598] The term “aroyl” embraces aryl radicals, as defined above,attached to an carbonyl radical as defined above. Examples of suchradicals include benzoyl and toluoyl.

[0599] The term “aralkanoyl” embraces aralkyl radicals, as definedherein, attached to an carbonyl radical as defined above. Examples ofsuch radicals include, for example, phenylacetyl.

[0600] The term “aralkoxy” embraces oxy-containing aralkyl radicalsattached through an oxygen atom to other radicals. More preferredaralkoxy radicals are “aralkoxy” radicals having phenyl radicalsattached to alkoxy radical as described above. Examples of such radicalsinclude benzyloxy, 1-phenylethoxy, 3-trifluoromethoxybenzyloxy,3-trifluoromethylbenzyloxy, 3,5-difluorobenyloxy, 3-bromobenzyloxy,4-propylbenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy, and2-phenyletboxy.

[0601] The term “aryloxyalkyl” embraces aryloxy radicals, as definedabove, attached to an alkyl group. Examples of such radicals includephenoxymethyl.

[0602] The term “haloaryloxyalkyl” embraces aryloxyalkyl radicals, asdefined above, wherein one to five halo radicals are attached to anaryloxy group.

[0603] The term “heteroaroyl” embraces heteroaryl radicals, as definedabove, attached to an carbonyl radical as defined above. Examples ofsuch radicals include furoyl and nicotinyl.

[0604] The term “heteroaralkanoyl” embraces heteroaralkyl radicals, asdefined herein, attached to an carbonyl radical as defined above.Examples of such radicals include, for example, pyridylacetyl andfurylbutyryl.

[0605] The term “heteroaralkoxy” embraces oxy-containing heteroaralkylradicals attached through an oxygen atom to other radicals. Morepreferred heteroaralkoxy radicals are “heteroaralkoxy” radicals havingheteroaryl radicals attached to alkoxy radical as described above. Theterm “heterocyclylalkoxy” embraces oxy-containing hetenocyclylalkylradicals attached through an oxygen atom to other radicals.

[0606] The term “haloheteroaryloxyalkyl” embraces heteroaryloxyalkylradicals, as defined above, wherein one to four halo radicals areattached to an heteroaryloxy group.

[0607] The term “heteroarylamino” embraces heteroaryl radicals, asdefined above, attached to an amino group. Examples of such radicalsinclude pyridylamino. The term “heterocyclylamino” embraces heterocyclylradicals, as defined above, attached to an amino group.

[0608] The term “heteroaralkylamino” embraces heteroaralkyl radicals, asdefined above, attached to an amino group. Examples of such radicalsinclude pyridylmethylamino. The term “heterocyclylaikylamino” embracesheterocyclylalkyl radicals, as defined above, attached to an aminogroup.

[0609] The term “heteroaryloxy” embraces heteroaryl radicals, as definedabove, attached to an oxy group. Examples of such radicals include2-thiophenyloxy, 2-pyrimidyloxy, 2-pyridyloxy, 3-pyridyloxy, and4-pyridyloxy. The term “heterocyclyloxy” embraces heterocyclyl radicals,as defined above, attached to an oxy group.

[0610] The term “heteroaryloxyalkyl” embraces heteroaryloxy radicals, asdefined above, attached to an alkyl group. Examples of such radicalsinclude 2-pyridyloxymethyl, 3-pyridyloxyethyl, and 4-pyridyloxymethyl.The term “heterocyclyloxyalkyl” embraces heterocyclyloxy radicals, asdefined above, attached to an alkyl group.

[0611] The term “arylthio” embraces aryl radicals, as defined above,attached to an sulfur atom. Examples of such radicals includephenylthio.

[0612] The term “arylthioalkyl” embraces arylthio radicals, as definedabove, attached to an alkyl group. Examples of such radicals includephenylthiomethyl.

[0613] The term “alkylthioalkyl” embraces alkylthio radicals, as definedabove, attached to an alkyl group. Examples of such radicals includemethylthiomethyl. The term “alkoxyalkyl” embraces alkoxy radicals, asdefined above, attached to an alkyl group. Examples of such radicalsinclude methoxymethyl.

[0614] The term “carbonyl” denotes a carbon radical having two of thefour covalent bonds shared with an oxygen atom. The term “carboxy”embraces a hydroxyl radical, as defined above, attached to one of twounshared bonds in a carbonyl group. The term “carboxamido” embracesamino, monoalkylamino, dialkylamino, monocycloalkylamino,alkylcycloalkylamino, dicycloalkylamino, N-alkyl-N-arylamino, arylamino,aralkyl amino, nitrogen containing heterocyclyl, heterocyclylamino,N-alkyl-N-heterocyclylamino, heteroarylamino, and heteroaralkylaminoradicals, attached to one of two unshared bonds in a carbonyl group. Theterm “carboxamidoalkyl” embraces carboxamido radicals, as defined above,attached to an alkyl group. The term “carboxyalkyl” embraces a carboxyradical, as defined above, attached to an alkyl group. The term“carboalkoxy” embraces alkoxy radicals, as defined above, attached toone of two unshared bonds in a carbonyl group. The term “carboaralkoxy”embraces aralkoxy radicals, as defined above, attached to one of twounshared bonds in a carbonyl group. The term “monocarboalkoxyalkyl”embraces one carboalkoxy radical, as defined above, attached to an alkylgroup. The term “dicarboalkoxyalkyl” embraces two carboalkoxy radicals,as defined above, attached to an alkylene group. The term“monocyanoalkyl” embraces one cyano, radical, as defined above, attachedto an alkyl group. The term “dicyanoalkylene” embraces two cyanoradicals, as defined above, attached to an alkyl group. The term“carboalkoxycyanoalkyl” embraces one cyano radical, as defined above,attached to an carboalkoxyalkyl group.

[0615] The term “acyl”, alone or in combination, means a carbonyl orthionocarbonyl group bonded to a radical selected from, for example,hydrido, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, alkoxyalkyl,haloalkoxy, aryl, heterocyclyl, heteroaryl, alkylsulfinylalkyl,alkylsulfonylalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl,alkylthio, arylthio, amino, alkylamino, dialkylamino, aralkoxy,arylthio, and alkylthioalkyl. Examples of “acyl” are formyl, acetyl,benzoyl, trifluoroacetyl, phthaloyl, malonyl, nicotinyl, and the like.The term “haloalkanoyl” embraces one or more halo radicals, as definedherein, attached to an alkanoyl radical as defined above. Examples ofsuch radicals include, for example, chloroacetyl, trifluoroacetyl,bromopropanoyl, and heptafluorobutanoyl.

[0616] The term “phosphono” embraces a pentavalent phosphorus attachedwith two covalent bonds to an oxygen radical. The term“dialkoxyphosphono” denotes two alkoxy radicals, as defined above,attached to a phosphono radical with two covalent bonds. The term“diaralkoxyphosphono” denotes two aralkoxy radicals, as defined above,attached to a phosphono radical with two covalent bonds. The term“dialkoxyphosphonoalkyl” denotes dialkoxyphosphono radicals, as definedabove, attached to an alkyl radical. The term “diaralkoxyphosphonoalkyl”denotes diaralkoxyphosphono radicals, as defined above, attached to analkyl radical.

[0617] The term “amino” denotes a nitrogen atom containing twosubstituents such as hydrido, hydroxy or alkyl and having one covalentbond available for bonding to a single atom such as carbon. Examples ofsuch amino radicals include, for example, —NH₂, —NHCH₃, —NHOH, and—NHOCH₃. The term “imino” denotes a nitrogen atom containing onesubstituent such as hydrido, hydroxy or alkyl and having two covalentbonds available for bonding to a single atom such as carbon. Examples ofsuch imino radicals include, for example, ═NH, ═NCH₃, ═NOH, and ═NOCH₃.The term “imino carbonyl” denotes a carbon radical having two of thefour covalent bond sites shared with an imino group. Examples of suchimino carbonyl radicals include, for example, C═NH, C═NCH₃, C═NOH, andC═NOCH₃. The term “amidino” embraces a substituted or unsubstitutedamino group bonded to one of two available bonds of an iminocarbonylradical. Examples of such amidino radicals include, for example,NH₂—C═NH, NH₂—C═NCH₃, NH₂—C═NOCH₃ and CH₃NH—C═NOH. The term “guanidino”denotes an amidino group bonded to an amino group as defined above wheresaid amino group can be bonded to a third group. Examples of suchguanidino radicals include, for example, NH₂—C(NH)—NH—, NH₂—C(NCH₃)—NH—,NH₂—C(NOCH₃)—NH—, and CH3NH—C(NOH)—NH—.

[0618] The term “sulfonium” denotes a positively charged trivalentsulfur atom where said sulfur is substituted with three carbon basedgroups such as alkyl, alkenyl, aralkyl, or aryl. The term “dialkylsulfonium” denotes a sulfonium group where said sulfur is substitutedwith two alkyl groups. Examples of such dialkylsulfonium radicalsinclude, for example, (CH₃)₂S⁺—. The term “dialkyl sulfonium alkyl”denotes a dialkyl sulfonium group where said group is bonded to one bondof an alkylene group as defined above. Examples of suchdialkylsulfoniumalkyl radicals include (CH₃)₂S⁺—CH₂CH₂—.

[0619] The term “phosphonium” denotes a positively charged tetravalentphosphorus atom where said phosphorus is substituted with four carbonbased groups such as alkyl, alkenyl, aralkyl, or aryl. The term“trialkyl phosphonium” denotes a phosphonium group where said phosphorusis substituted with three alkyl groups. Examples of suchtrialkylphosphonium radicals include, for example, (CH₃)₃P⁺—.

[0620] Said “alkyl”, “alkenyl”, “alkynyl”, “alkanoyl”, “alkylene”,“alkenylene”, “hydroxyalkyl”, “haloalkyl”, “haloalkylene”,“haloalkenyl”, “alkoxy”, “alkenyloxy”, “alkenyloxyalkyl”, “alkoxyalkyl”,“aryl”, “perhaloaryl”, “haloalkoxy”, “haloalkoxyalkyl”,“haloalkenyloxy”, “haloalkenyloxyalkyl”, “alkylenedioxy”,“haloalkylenedioxy”, “heterocyclyl”, “heteroaryl”, “hydroxyhaloalkyl”,“alkylsulfonyl”, “haloalkyl sulfonyl”, “alkylsulfonylalkyl”, “haloalkylsulfonylalkyl”, “alkylsulfinyl”, “alkylsulfinylalkyl”,“haloalkylsulfinylalkyl”, “aralkyl”, “heteroaralkyl”, “perhaloaralkyl”,“aralkylsulfonyl”, “aralkylsulfonylalkyl”, “aralkylsulfinyl”,“aralkylsulfinylalkyl”, “cycloalkyl”, “cycloalkylalkanoyl”,“cycloalkylalkyl”, “cycloalkenyl”, “halocycloalkyl”, “halocycloalkenyl”,“cycloalkylsulfinyl”, “cycloalkylsulfinylalkyl”, “cycloalkyl sulfonyl”,“cycloalkylsulfonylalkyl”, “cycloalkoxy”, “cycloalkoxyalkyl”,“cycloalkylalkoxy”, “cycloalkenyloxy”, “cycloalkenyloxyalkyl”,“cycloalkylenedioxy”, “halocycloalkoxy”, “halocycloalkoxyalkyl”,“halocycloalkenyloxy”, “halocycloalkenyloxyalkyl”, “alkylthio”,“haloalkylthio”, “alkylsulfinyl”, “amino”, “oxy”, “thio”, “alkylamino”,“arylamino”, “aralkyl amino”, “arylsulfinyl”, “arylsulfinylalkyl”,“arylsulfonyl”, “arylsulfonylalkyl”, “heteroarylsulfinyl”,“heteroarylsulfinylalkyl”, “heteroarylsulfonyl”,“heteroarylsulfonylalkyl”, “heteroarylamino”, “heteroaralkylamino”,“heteroaryloxy”, “heteroaryloxylalkyl”, “aryloxy”, “aroyl”,“aralkanoyl”, “aralkoxy”, “aryloxyalkyl”, “haloaryloxyalkyl”,“heteroaroyl”, “heteroaralkanoyl”, “heteroaralkoxy”,“heteroaralkoxyalkyl”, “arylthio”, “arylthioalkyl”, “alkoxyalkyl”,“acyl”, “amidino”, “guanidino”, “dialkylsulfonium”,“trialkylphosphonium”, and “dialkylsulfoniumalkyl” groups defined abovemay optionally have 1 or more non-hydrido substituents such as amidino,guanidino, dialkylsulfonium, trialkylphosphonium, dialkylsulfoniumalkyl,perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl,aralkylsulfinylalkyl halocycloalkyl, halocycloalkenyl,cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl,cycloakylsulfonylalkyl, heteroarylamino, N-heteroarylamino-N-alkylamino,heteroaralkylamino, heteroaryloxy, heteroaryloxylalkyl, haloalkylthio,alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy,cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy,cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy,halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl,hydroxy, amino, thio, nitro, alkylamino, alkylthio, alkylthioalkyl,arylamino, aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl,alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfonylalkyl,heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl,alkylsulfonylalkyl, haloalkylsulfinylalkyl, haloalkylsulfonylalkyl,alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkylamidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl,arylsulfonamido, diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl,arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl,heteroarylsulfonyl, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl,heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy,alkenyloxyalky, alkylenedioxy, haloalkylenedioxy, cycloalkyl,cycloalkylalkanoyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl,halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl,hydroxyaralkyl, hydroxyalkyl, aminoalkyl, hydoxyheteroaralkyl,haloalkoxyalkyl, aryl, aralkyl, aryloxy, aralkoxy, aryloxyalkyl,saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl,heteroaryloxy, heteroaryloxyalkyl, arylalkyl, heteroaralkyl,arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy,alkoxycarbonyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano,carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, anddiaralkoxyphosphonoalkyl.

[0621] The term “spacer” can include a covalent bond and a linear moietyhaving a backbone of 1 to 7 contiguous atoms. The spacer may have 1 to 7atoms of a univalent or multi-valent chain. Univalent chains may beconstituted by a radical selected from ═C(H)—, ═C(R^(2a))—, —O—, —S—,—S(O)—, —S(O)₂—, —NH—, —N(R^(2a))—, —N═, —CH(OH)—, ═C(OH)—,—CH(OR^(2a))—, ═C(OR^(2a))—, and —C(O)— wherein R^(2a) is selected fromalkyl, alkenyl, alkynyl, aryl, heteroaryl, aralkyl, aryloxyalkyl,alkoxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl,haloalkyl, haloalkenyl, haloalkoxyalkyl, perhaloaralkyl,heteroarylalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, andheteroarylalkenyl. Multi-valent chains may consist of a straight chainof 1 or 2 or 3 or 4 or 5 or 6 or 7 atoms or a straight chain of 1 or 2or 3 or 4 or 5 or 6 atoms with a side chain. The chain may beconstituted of one or more radicals selected from: alkylene, alkenyl,—O—, —O—CH₂—, —S—CH₂—, —CH₂CH₂—, ethenyl, —CH═CH(OH)—, —OCH₂O—,—O(CH₂)₂O—, —NHCH₂—, —OCH(R^(2a))O—, —O(CH₂CHR^(2a))O—, —OCF₂O—,—O(CF₂)₂O—, —S—, —S(O)—, —S(O)₂—, —N(H)—, —N(H)O—, —N(R^(2a))O—,—N(R^(2a))—, —C(O)—, —C(O)NH—, —C(O)NR^(2a)—, —N═, —OCH₂—, —SCH₂—,S(O)CH₂—, —CH₂C(O)—, —CH(OH)—, ═C(OH)—, —CH(OR²)—, ═C(OR^(2a))—,S(O)₂CH₂—, and —NR^(2a)CH₂— and many other radicals defined above orgenerally known or ascertained by one of skill-in-the art. Side chainsmay include substituents such as 1 or more non-hydrido substituents suchas amidino, guanidino, dialkylsulfonium, trialkylphosphonium,dialkylsulfoniumalkyl, perhaloaralkyl, aralkylsulfonyl,aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl,halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl,cycloalkylsulfinylalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl,heteroarylamino, N-heteroaryl amino-N-alkylamino, heteroaralkylamino,heteroaryloxy, heteroaryloxylalkyl, haloalkylthio, alkanoyloxy, alkoxy,alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy,cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy,cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy,halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl,hydroxy, amino, thio, nitro, alkylamino, alkylthio, alkylthioalkyl,arylamino, aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl,alkylsulfinyl, alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfonylalkyl,heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl,alkylsulfonylalkyl, haloalkylsulfinylalkyl, haloalkylsulfonylalkyl,alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkylamidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl,arylsulfonamido, diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl,arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl,heteroarylsulfonyl, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl,heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy,alkenyloxyalky, alkylenedioxy, haloalkylenedioxy, cycloalkyl,cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, halo, haloalkyl,haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl,aminoalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, aralkyl,aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl, partiallysaturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl,arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl,carboxyalkyl, carboalkoxy, carboaralkoxy, carboxamido, carboxamidoalkyl,cyano, carbohaloalkoxy, phosphono, phosphonoalkyl, diarailkoxyphosphono,and diaralkoxypbosphonoalkyl.

[0622] Compounds of the present invention can exist in tautomeric,geometric or stereoisomenic forms. The present invention contemplatesall such compounds, including cis- and trans-geometric isomers, E- andZ-geometric isomers, R- and S-enantiomers, diastereomers, d-isomers,1-isomers, the racemic mixtures thereof and other mixtures thereof, asfalling within the scope of the invention. Pharmaceutically acceptablesales of such tautomeric, geometric or stereoisomeric forms are alsoincluded within the invention.

[0623] The terms “cis” and “trans” denote a form of geometric isomerismin which two carbon atoms connected by a double bond will each have ahydrogen atom on the same side of the double bond (“cis”) or on oppositesides of the double bond (“trans”).

[0624] Some of the compounds described contain alkenyl groups, and aremeant to include both cis and trans or “E” and “Z” geometric forms.

[0625] Some of the compounds described contain one or more stereocentersand are meant to include R, S, and mixtures of R and S forms for eachstereocenter present.

[0626] Some of the compounds described herein may contain one or moreketonic or aldehydic carbonyl groups or combinations thereof alone or aspart of a heterocyclic ring system. Such carbonyl groups may exist inpart or principally in the “keto” form and in part or principally as oneor more “enol” forms of each aldehyde and ketone group present.Compounds of the present invention having aldehydic or ketonic carbonylgroups are meant to include both “keto” and “enol” tautomeric forms.

[0627] Some of the compounds described herein may contain one or moreamide carbonyl groups or combinations thereof alone or as part of aheterocyclic ring system. Such carbonyl groups may exist in part orprincipally in the “keto” form and in part or principally as one or more“enol” forms of each amide group present. Compounds of the presentinvention having amidic carbonyl groups are meant to include both “keto”and “enol” tautomeric forms. Said amide carbonyl groups may be both oxo(C═O) and thiono (C═S) in type.

[0628] Some of the compounds described herein may contain one or moreimine or enamine groups or combinations thereof. Such groups may existin part or principally in the “imine” form and in part or principally asone or more “enamine” forms of each group present. Compounds of thepresent invention having said imine or enamine groups are meant toinclude both “imine” and “enamine” tautomeric forms.

[0629] The present invention also comprises a treatment and prophylaxisin anticoagulant therapy for the treatment and prevention of a varietyof thrombotic conditions including coronary artery and cerebrovasculardisease in a subject, comprising administering to the subject havingsuch disorder a therapeutically-effective amount of a compound ofFormula (I):

[0630] or a pharmaceutically-acceptable salt thereof.

[0631] As a further embodiment, compounds of the present invention ofFormula (I) or a pharmaceutically-acceptable salt thereof as definedabove, comprise a treatment and prophylaxis of coronary artery disease,cerebrovascular disease and other coagulation cascade related disordersin a subject, comprising administering to the subject having suchdisorder a therapeutically-effective amount of compounds of formula (I)of the present invention or a pharmaceutically-acceptable salt thereof.

[0632] Compounds of the present invention of Formula (I) or apharmaceutically-acceptable salt thereof can also be used wheneverinhibition of blood coagulation is required such as to preventcoagulation of stored whole blood and to prevent coagulation in otherbiological samples for testing or storage. Thus coagulation inhibitorsof the present inhibition can be added to or contacted with stored wholeblood and any medium containing or suspected of containing plasmacoagulation factors and in which it is desired that blood coagulation beinhibited, e.g. when contacting the mammal's blood with materialselected from the group consisting of vascular grafts, stents,orthopedic prothesis, cardiac prosthesis, and extracorporeal circulationsystems.

[0633] Compounds of Formula (I) are capable of inhibiting activity ofserine proteases related to the coagulation cascade, and thus could beused in the manufacture of a medicament, a method for the prophylacticortherapeutic treatment of diseases mediated by coagulation cascadeserine proteases, such as inhibiting the formation of blood plateletaggregates, inhibiting the formation of fibrin, inhibiting thrombusformation, and inhibiting embolus formation in a mammal, in blood, inblood products, and imammalian organs. The compounds also can be usedfor treating or preventing unstable angina, refractory angina,myocardial infarction, transient ischemic attacks, atrial fibrillation,thrombotic stroke, embolic stroke, deep vein thrombosis, disseminatedintravascular coagulation, ocular build up of fibrin, and reocclusion orrestenosis of recanalized vessels in a mammal. The compounds also can beused to study the mechanism of action of coagulation cascade serineproteases to enable the design of better inhibitors and development ofbetter assay methods. The compounds of Formula (I) would be also usefulin prevention of cerebral vascular accident (CVA) or stroke.

[0634] Also included in the family of compounds of Formula (I) are thepharmaceutically-acceptable salts thereof. The term“pharmaceutically-acceptable salt” embraces salts commonly used to formalkali metal salts and to form addition salts of free acids or freebases. The nature of the salt is not critical, provided that it ispharmaceutically acceptable. Suitable pharmaceutically-acceptable acidaddition salts of compounds of Formula (I) may be prepared frominorganic acid or from an organic acid. Examples of such inorganic acidsare hydrochloric, hydrobromic, hydroiodic, nitric, carbonic, sulfuricand phosphoric acid. Appropriate organic acids may be selected fromaliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic,carboxylic and sulfonic classes of organic acids, examples of which areformic, acetic, propionic, succinic, glycolic, gluconic, lactic, malic,tartaric, citric, ascorbic, glucoronic, maleic, fumaric, pyruvic,aspartic, glutamic, benzoic, anthranilic, mesylic, salicylic,p-hydroxybenzoic, phenylacetic, mandelic, embonic (pamoic),methanesulfonic, ethylsulfonic, benzenesulfonic, sulfanllic, stearic,cyclohexylaminosulfonic, algenic, galacturonic acid. Suitablepharmaceutically-acceptable base addition salts of compounds of Formula(I) include metallic salts made from aluminum, calcium, lithium,magnesium, potassium, sodium and zinc or organic salts made fromN,N′-dibenzylethyleneldiamine, choline, chloroprocaine, diethanolamine,ethylenediamine, meglumine (N-methylglucamine) and procain. All of thesesalts may be prepared by conventional means from the correspondingcompound of Formula (I) by reacting, for example, the appropriate acidor base with the compound of Formula (I).

[0635] The present invention also comprises a pharmaceutical compositioncomprising a therapeutically-effective amount of a compound of Formulas(I) in association with at least one pharmaceutically-acceptablecarrier, adjuvant or diluent. Pharmaceutical compositions of the presentinvention can comprise the active compounds of Formula (I) inassociation with one or more non-toxic, pharmaceutically-acceptablecarriers and/or diluents and/or adjuvants (collectively referred toherein as “carrier” materials) and, if desired, other activeingredients. The active compounds of the present invention may beadministered by any suitable route, preferably in the form of apharmaceutical composition adapted to such a route, and in a doseeffective for the treatment intended.

[0636] The active compounds and composition may, for example, beadministered orally, intravascularly, intraperitoneally, subcutaneously,intramuscularly, oculary, or topically. For treating ocular build up offibrin, the compounds may be administered intraocularly or topically aswell as orally or parenterally.

[0637] The compounds can be administered in the form of a depotinjection or implant preparation which may be formulated in such amanner as to permit a sustained release of the active ingredient. Theactive ingredient can be compressed into pellets or small cylinders andimplanted subcutaneously or intramusculary as depot injections orimplants. Implants may employ inert materials such as biodegradablepolymers or synthetic silicones, for example, Silastic, silicone rubberor other silicon containing polymers.

[0638] The compounds can also be administered in the form of liposomedelivery systems, such as small unilamellar vesicles, large unilamellarvesicles and multilamellar vesicles. Liposomes can be formed from avariety of phospholipids, such as cholesterol, stearylamine orphosphatidylcholines.

[0639] The compounds may also be delivered by the use of monoclonalantibodies as individual carriers to which the compound molecules arecoupled. The compounds may also be coupled with soluble polymers astargetable drug carriers. Such polymers can includepclyvinylpyrrolidone, pyran copolymer,polyhydroxy-propyl-methacrylamide-phenol,polyhydroxyethyl-aspartamide-phenol, or ployethyleneoxide-polylysinesubstituted with palmitoyl residues. Furthermore, the compounds may becoupled to a class of biodegradable polymers useful in achievingcontrolled release of a drug, for example, polylactic acid, polyglycolicacid, copolymers of polylactic and polyglycolic acid, polyepsiloncaprolactone, polyhydroxy butyric acid, polyorthoesters, polyacetals,polydihydropyrans, polycyanoacrylates and cross linked or amphitpathicblock copolymers of hydrogels.

[0640] For oral administration, the pharmaceutical composition may be inthe form of, for example, tablets, capsules (each of which includessustained release or timed release formulations), pills, powders,granules, elixers, tinctures, suspensions, liquids including syrups, andemulsions. The pharmaceutical composition is preferably made in the formof a dosage unit containing a particular amount of the activeingredient. Examples of such dosage units are tablets or capsules. Theactive ingredient may also be administered by injection as a compositionwherein, for example, saline, dextrose or water may be used as asuitable carrier.

[0641] The amount of therapeutically active compounds which areadministered and the dosage regimen for treating a disease conditionwith the compounds and/or compositions of this invention depends on avariety of factors, including the age, weight, sex and medical conditionof the subject, the severity of the disease, the route and frequency ofadministration, and the particular compound employed, and thus may varywidely.

[0642] The pharmaceutical compositions may contain active ingredients inthe range of about 0.1 to 2000 mg, and preferably in the range of about0.5 to 500 mg. A daily dose of about 0.01 to 100 mg/kg body weight, andpreferably between about 0.5 and about 20 mg/kg body weight, may beappropriate. The daily dose can be administered in one to four doses perday.

[0643] The compounds may be formulated in topical ointment or cream, oras a suppository, containing the active ingredients in a total amountof, for example, 0.075 to 30% w/w, preferably 0.2 to 20% w/w and mostpreferably 0.4 to 15% w/w. When formulated in an ointment, the activeingredients may be employed with either paraffinic or a water-miscibleointment base.

[0644] Alternatively, the active ingredients may be formulated in acream with an oil-in-water cream base. If desired, the aqueous phase ofthe cream base may include, for example at least 30% w/w of a polyhydricalcohol such as propylene glycol, butane-1,3-diol, mannitol, sorbitol,glycerol, polyethylene glycol and mixtures thereof. The topicalformulation may desirably include a compound which enhances absorptionor penetration of the active ingredient through the skin or otheraffected areas. Examples of such dermal penetration enhancers includedimethylsulfoxide and related analogs. The compounds of this inventioncan also be administered by a transdermal device. Preferably topicaladministration will be accomplished using a patch either of thereservoir and porous membrane type or of a solid matrix variety. Ineither case, the active agent is delivered continuously from thereservoir or microcapsules through a membrane into the active agentpermeable adhesive, which is in contact with the skin or mucosa of therecipient. If the active agent is absorbed through the skin, acontrolled and predetermined flow of the active agent is administered tothe recipient. In the case of microcapsules, the encapsulating agent mayalso function as the membrane.

[0645] The oily phase of the emulsions of this invention may beconstituted from known ingredients in a known manner. While the phasemay comprise merely an emulsifier, it may comprise a mixture of at leastone emulsifier with a fat or an oil or with both a fat and an oil.Preferably, a hydrophilic emulsifier is included together with alipophilic emulsifier which acts as a stabilizer. It is also preferredto include both an oil and a fat. Together, the emulsifier(s) with orwithout stabilizer(s) make up the so-called emulsifying wax, and the waxtogether with the oil and fat make up the so-called emulsifying ointmentbase which forms the oily dispersed phase of the cream formulations.Emulsifiers and emulsion stabilizers suitable for use in the formulationof the present invention include Tween 60, Span 80; cetostearyl alcohol,myristyl alcohol, glyceryl monostearate, and sodium lauryl sulfate,among others.

[0646] The choice of suitable oils or fats for the formulation is basedon achieving the desired cosmetic properties, since the solubility ofthe active compound in most oils likely to be used in pharmaceuticalemulsion formulations is very low. Thus, the cream should preferably bea non-greasy, non-staining and washable product with suitableconsistency to avoid leakage from tubes or other containers. Straight orbranched chain, mono- or dibasic alkyl esters such as diisoadipate,isocetyl stearate, propylene glycol diester of coconut fatty acids,isopropyl myristate, decyl oleate, isopropyl palmitate, butyl stearate,2-ethylhexyl palmitate or a blend of branched chain esters may be used.These may be used alone or in combination depending on the propertiesrequired. Alternatively, high melting point lipids such as white softparaffin and/or liquid paraffin or other mineral oils can be used.

[0647] For therapeutic purposes, the active compounds of the presentinvention are ordinarily combined with one or more adjuvants appropriateto the indicated route of administration. If administered per os, thecompounds may be admixed with lactose, sucrose, starch powder, celluloseesters of alkanoic acids, cellulose alkyl esters, talc, stearic acid,magnesium stearate, magnesium oxide, sodium and calcium salts ofphospboric and sulfuric acids, gelatin, acacia gum, sodium alginate,polyvinylpyrrolidone, and/or polyvinyl alcohol, and then tableted orencapsulated for convenient administration. Such capsules or tablets maycontain a controlled-release formulation as may be provided in adispersion of active compound in hydroxypropylmethyl cellulose.Formulations for parenteral administration may be in the form of aqueousor non-aqueous isotonic sterile injection solutions or suspensions.These solutions and suspensions may be prepared from sterile powders orgranules having one or more of the carriers or diluents mentioned foruse in the formulations for oral administration. The compounds may bedissolved in water, polyethylene glycol, propylene glycol, ethanol, cornoil, cottonseed oil, peanut oil, sesame oil, benzyl alcohol, sodiumchloride, and/or various buffers. Other adjuvants and modes ofadministration are well and widely known in the pharmaceutical art.

[0648] In practicing the methods of the present invention for thetreatment and prevention of a variety of thrombotic conditions includingcoronary artery and cerebrovascular disease, the compounds andpharmaceutical compositions of the present invention are administeredalone or in combination with one another, or in combination with othertherapeutics or in vivo diagnostic agents. The coagulation cascadeinhibitors of the present invention can also be co-administered withsuitable anti-platelet agreggation agents, including, but not limited toticlopidine or clopidrogel, fibrinogen receptor antagonists (e.g. totreat or prevent unstable angina or to prevent reocculsion afterangioplasty and restenosis), anti-coagulants such as aspirin, warfarinor heparins, thrombolytic agents such as plasminogen activators orstreptokinase to achieve synergistic effects in the treatment of variouspathologies, lipid lowering agents including, antihypercholesterolemics(e.g. HMG CoA reductase inhibitors such as mevastatin, lovastatin,simvastatin, pravastatin, and fluvastatin, HMG CoA synthataseinhibitors, etc.), anti-diabetic drugs, or other cardiovascular agents(loop diuretics, thiazide type diuretics, nitrates, aldosteroneantagonistics (i.e., spironolactone and epoxymexlerenone), angiotensinconverting enzyme (e.g. ACE) inhibitors, angiotensin II receptorantagonists, beta-blockers, antiarrythmics, anti-hypertension agents,and calcium channel blockers) to treat or prevent atheriosclerosis. Forexample, patients suffering from coronary artery disease, and patientssubjected to angioplasty procedures, would benefit from coadministrationof fibrinogen receptor antagonists and coagulation cascade inhibitors ofthe present invention. Also, coagulation cascade inhibitors couldenhance the efficiency of tissue plasminogen activator-mediatedthrombolytic reperfusion.

[0649] Typical doses of coagulation cascade inhibitors of the presentinvention with other suitable anti-platelet agents, anticoagulationagents, cardiovascular therapeutic agents, or thrombolytic agents may bethe same as those doses of coagulation cascade inhibitors administeredwithout coadministration of additional anti-platelet agents,anticoagulation agents, cardiovascular therapeutic agents, orthrombolytic agents, or may be substantially less than those doses ofcoagulation cascade inhibitors administered without coadministration ofadditional anti-platelet agents, anticoagulation agents, cardiovasculartherapeutic agents, or thrombolytic agents, depending on a patient'stherapeutic needs.

[0650] The present novel methods preferably employ compounds whichselectively inhibit human TF-VIIA over the inhibition of both humanThrombin II and human factor Xa. Preferably, the compounds have a humanTF-VIIA IC₅₀ of less than 0.5 μM and also have a selectivity ratio ofTF-VIIA inhibition over both human Thrombin II and human factor Xainhibition of at least 10, and more preferably at least 100. Even morepreferably, the compounds have a human TF-VIIA IC₅₀ of less than 0.1 μmand also have a selectivity ratio of TF-VIIA inhibition ovca both humanThrombin 11 and human factor Xa inhibition of at least 1000, and mostpreferably at least 10,000.

[0651] All mentioned references are incorporated by reference as if herewritten.

[0652] Although this invention has been described with respect tospecific embodiments, the details of these embodiments are not to beconstrued as limitations. The following examples are provided toillustrate the present invention and are not intended to limit the scopethereof. Without further elaboration, it is believed that one skilled inthe art can, using the preceding descriptions, utilize the presentinvention to its fullest extent. Therefore the following preferredspecific embodiments are to be construed as merely illustrative and notlimitative of the remainder of the disclosure in any way whatsoever.Compounds containing multiple variations of the structural modificationsillustrated in the schemes or the following Examples are alsocontemplated. Those skilled in the art will readily understand thatknown variations of the conditions and processes of the followingpreparative procedures can be used to prepare these compounds.

[0653] One skilled in the art may use these generic methods to preparethe following specific examples, which have been or may be properlycharacterized by ¹H NMR, mass spectrometry, elemental composition, andsimilar procedures. These compounds also may be formed in vivo.

[0654] The following examples contain detailed descriptions of themethods of preparation of compounds of Formula (1). These detaileddescriptions fall within the scope and are presented for illustrativepurposes only and are not intended as a restriction on the scope of theinvention. All parts are by weight and temperatures are Degreescentigrade unless otherwise indicated.

[0655] The following general synthetic sequences are useful in makingthe present invention. Abbreviations used in the schemes are as follows:“AA” represents amino acids, “AcCN” represents acetonitrile, “AcOH”represents acetic acid, “BINAP” represents2,2′-bis(diphenylphosphino)-1,1′-binaphthyl, “BnOH” represents benzylalcohol, “BnCHO” represents 2-phenylethanal, “BnSO₂Cl” representsbenzylsulfonyl chloride, “Boc” represents tert-butyloxycarbonyl, “BOP”represents benzotriazol-1-yl-oxy-tris-(dimethylamino), “bu” representsbutyl, “dba” represents dibenzylideneacetone, “DCC” represents1,3-dicyclohexylcarbodiimide, “DCM” represents dichloromethane ormethylene chloride, “DIBAH” or “DIBAL” represents diisobutylaluminumhydride, “DMF” represents dimethylformamide, “DMSO” representsdimethylsulfoxide, “DPPA” represents diphenylphosphoryl azide”, “EDC”represents 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimidehydrochloride, “Fmoc” represents 9-fluorenylmethoxycarbonyl, “HOBt”represents hydroxybenzoltriazole”, “LDA” represents lithiumdiisopropylamide, “NMM” represents N-methylmorpholine, “Ph” representsphenyl or aryl, “PHTH” represents a phthaloyl group, “pnZ” represents4-nitrobenzyloxycarbonyl, “PFC” represents a phase transfer catalyst,“py” represents pyridine, “RNH2” represents a primary organic amine,“p-TsOH” represents paratoluenesulfonic acid, “TBAF” representstetrabutylammonium fluoride, “TBTU” represents2-(1H-benzotriozole-1-yl)-1,1,3,3-tetramethyl uronium tetrafluoroborate,“TEA” represents triethylamine, “TFA” represents trifluoroacetic acid,“HF” represents tetrahydrofuran, “MS” represents trimethylsilyl, “TMSCN”represents trimethylsilyl cyanide, and “Cbz” or “Z” representsbenzyloxycarbonyl.

GENERAL SYNTHETIC PROCEDURES AND SPECIFIC EXAMPLES

[0656] The benzene compounds of the present invention can besynthesized, for example, according to the following procedures andSchemes given below. Schemes 1 and 2 below summarize generic proceduresthat permit the preparation of a wide variety of the compounds of thepresent invention through the ability to introduce numerous R²substituents represented by Z⁰-Q, a wide variety of amino substitutinggroups represented by B-A, and a large number of amide forming Y groupsat the carboxylic acid group in which K is a covalent single bond.

[0657] Example 1 below shows the preparation of a compound wherein X⁰,R¹, and J are each hydrido.

Example 1

[0658]

[0659] Triethylamine (8.3 mL, 0.060 mol) was added to a solution of2-fluoro-5-nitrobenzoic acid (5.0 g, 0.027 mol) and thiophenol (2.8 mL,0.027 mol) in tetrahydrofuran. After stirring at reflux for 20 hours, asaturated solution of ammonium chloride was added until solution becameneutral. The solution was extracted with dichloromethane and the organiclayer was washed with water, brine, dried over magnesium sulfate, andfiltered. The solvent was removed by evaporation to afford 8.85 g (87%)of a yellow solid of product EX-1A; ¹H NMR ppm: 1.40 (t, 9H), 3.21 (q,6H), 6.75 (d, 1H, J=8.7 Hz), 7.47 (m, 3H), 7.57 (m, 2H), 7.85 (d, 1H,J=8.7 Hz), 8.85 (d, 1H, J=2.4 Hz).

[0660] Oxalyl chloride (7.7 mL, 0.088 mol) was added to a solution ofthe acid EX-1A (−6.68 g, 0.017 mol) in dichloromethane followed by adrop of dimethylformamide. After stirring at room temperature for 1hour, the solvent was removed by evaporation to afford the acidchloride. The acid chloride was redissolved into dichloromethane and anexcess of methanol (50 mL) was added followed by addition of pyridine(2.0 mL, 0.024 mol). The solution stirred at room temperature for 2.5hours. The solution was washed with water, brine, dried over magnesiumsulfate, and filtered. The solvent was removed by evaporation to affordthe crude product. The product was purified by column chromatography(30% ethyl acetate-hexane) to afford 4.21 g (82%) of a yellow solid ofproduct EX-1B; ¹H NMR ppm: 4.05 (s, 3H), 6.89 (d, 1H, J=9.0 Hz), 7.61(m, 5H), 8.05 (dd, 1H, J=8.7,2.4 Hz), 8.88 (d, 1H, J=2.4 Hz); HRMS calcdfor C₁₄H₁₁O₄N₁S₁ (M⁺+H) 290.0487, found 290.0491.

[0661] The nitro compound EX-1B (3.71 g, 0.012 mmol) was stirred inglacial acetic acid. Powdered iron (3.58 g, 0.064 mmol) was added andthe solution was heated to 80° C. with vigorous stirring. The solutionwas stirred at 80° C. for 15 minutes at which point the iron had turnedgray. The reaction mixture was filtered through celite and the solid waswashed with ether. The resultant organic layer was washed with water,stirred with saturated sodium bicarbonate until basic, and washed withwater again. The solution was dried over magnesium sulfate, filtered andthe solvent was removed to afford 2.48 g (75%) of a yellow oil ofproduct EX-1C; 1H NMR ppm: 3.90 (s, 3H), 6.89 (dd, 1H, J=8.4, 2.7 Hz),6.96 (d, 1H, J=8.4 Hz), 7.22 (d, 1H, J=2.7 Hz), 7.32 (m, 5H); HPLCpurity (retention time): >99% (2.81 min); HRMS calcd for C₁₄H₁₃O₂N₁S₁(M⁺+H) 260.0745, found 260.0718.

[0662] Diisopropylethylamine (2.5 mL, 1.42 mmol) was added to a solutionof the aniline EX-1C (2.46 g, 9.48 mmol) and a-toluenesulfonyl chloride(3.17 g, 16.6 mmol) in dichloromethane, and the resulting solutionstirred at room temperature for 3 hours. The solution was washed with 2N hydrochloric acid, brine, dried over magnesium sulfate, and filtered.The solvent was removed by evaporation to afford a mixture of twoproducts. Fraction one of column chromatography (30% ethylacetate-hexane) afforded 2.64 g (49%) of a white solid of product EX-1D;¹H NMR ppm: 3.94 (s, 3H), 4.85 (s, 4H), 6.22 (dd, 1H, J=9.0, 2.4 Hz),6.44 (d, 1H, J=9.0 Hz), 7.07 (d, 1H, J=2.4 Hz), 7.40 (m, 7H), 7.50 (m,9H); HRMS calcd for C₂₈H₂₅O₆N₁S₃ (M⁺+NH₄) 585.1188, found 585.1141.

[0663] Following the same procedure described for EX-1D, fraction two ofcolumn chromatography (30% ethyl acetate-hexane) afforded 1.16 g (30%)of a white solid of product EX-1E; ¹H NMR ppm: 3.98 (s, 3H), 4.32 (s,2H), 6.66 (s, 1H), 6.80 (d, 1H), 7.28 (dd, 1H), 7.29-7.73 (m, 11H); HPLCpurity (retention time): 97.2% (4.20 min); HRMS calcd for C₂₁H₁₉O₄N₁S₂(M⁺+NH₄) 431.1099, found 431.1069.

[0664] Aqueous sodium hydroxide (10%) (3.0 mL, 7.5 mmol) was added to asolution of the methyl ester EX-1E (0.70 g, 1.7 mmol) in methanol andthe resulting solution stirred at 65° C. for 4 hours. The solution wasacidified with 2 N hydrochloric acid and extracted with ether. Thesolution was washed with brine, dried over magnesium sulfate, andfiltered. The solvent was removed by evaporation to afford 0.66 g (98%)of a white solid of product EX-1F; ¹H NMR ppm: 3.86 (s, 2H), 6.31 (dd,1H), 6.83 (m, 6H), 6.97 (m, 3H), 7.06 (m, 2H), 7.52 (d, 1H), 9.35 (s,1H); HPLC purity (retention time): 93.9% (3.69 min); HRMS calcd forC₂₀H₁₇O₄N₁S₂ (M⁺+NH₄) 417.0943, found 417.0933.

[0665] Under conditions of parallel reaction synthesis,1-hydroxybenzotriazole (16.2 mg, 0.12 mmol) was added to a slurry of theacid EX-1F (47.9 mg, 0.12 mmol) and PolyStyrenyl-carbodiimide (PSDCC)(1.00 mmol/g) (200 mg, 0.20 mmol) in 3 mL of dichloromethane and 0.5 mLof dimethylformamide. The suspension was agitated for 15 minutes. Theamine, N-Boc-piperidin-4-ylmethylamine (0.10 mmol) was added,N-methylmorpholine (13.1 μL, 0.12 mmol) was added when the amine is ahydrochloride salt, and the suspension was agitated for 2 hours. Uponcompletion of the reaction, the polyamine resin (PSA) (2.69 mmol/g)(0.40 g, 1.0 mmol) and polymer-bound aldehyde (PSCHO) (2.3 mmol/g) (0.43g, 1.0 mmol) was added and the suspension was agitated for 3 hours. Thesolution was filtered and the polymer was rinsed with dimethylformamideand dichloromethane until no more UV activity was seen in thedichloromethane washing. The combined filtrate and washings wereevaporated to afford the pure product EX-1G.

[0666] Under conditions of parallel reaction synthesis, hydrochloricacid in dioxane (4N) (3 mL) was added to the Boc protected compoundEX-1G, and the solution was agitated at room temperature for 19 hours.Evaporation of the solvents afforded 58.4 mg (98%) of a clear oil ofproduct; ¹H NMR ppm: 1.21 (m, 2H), 1.45 (s, 9H), 1.62 (m, 3H), 2.63 (m,2H), 3.25 (m, 2H), 4.03 (m, 2H), 4.35 (s, 2H), 7.27 (m, 13H), 7.66 (s,1H); HPLC purity (retention time): >99% (4.41 min).

Example 2

[0667]

[0668] Using the procedure of Example 1, use of4-dimethylaminobenzylamine afforded 30.0 mg (70%) of a white solid ofproduct; ¹H NMR ppm: 2.95 (s, 6H), 4.35 (s, 2H), 4.44 (d, 2H), 6.70 (d,2H), 7.23 (m, 16H), 7.62 (s, 11H); HPLC purity (retention time): >99%(3.15 min); HRMS calcd for C₂₉H₂₉O₃N₃S₂ (M⁺+H) 532.1729, found 532.1681.

Example 3

[0669]

[0670] Using the procedure of Example 1, use of 4-pyridymethylamineafforded 30.5 mg (62%) of a white solid of product; ¹H NMR ppm: 4.35 (s,2H), 4.55 (d, 2H), 7.13 (d, 2H), 7.26 (m, 13H), 7.66 (s, 2H), 8.39 (d,2H); HPLC purity (retention time): >99% (3.00 min); HRMS calcd forC₂₆H₂₃O₃N₃S₂ (M⁺+H) 490.1259, found 490.1222.

Example 4

[0671]

[0672] Using the procedures of Example 1 and4-(N-Boc-amidino)benzylamine, 89.9 mg (71%) of a clear oil of productEX-4A was produced; ¹H NMR ppm: 1.56 (s, 9H), 4.31 (s, 2H), 4.52 (d,2H), 7.12-7.68 (m, 19H); HPLC purity (retention time): 66.4% (3.41 min).

[0673] Using the procedures of Example 1, EX-4A afforded 89.9 mg (71%)of a clear oil of product; ¹H NMR ppm: 4.85 (s, 2H), 4.90 (d, 2H),7.52-8.22 (m, 18H), 9.31 (m, 1H), 9.82 (bs, 1H), 10.22 (s, 1H), 10.49(s, 1H); HPLC purity (retention time): >83.7% (3.15 min); HRMS calcd forC₂₈H₂₆O₃N₄S₂ (M⁺+H) 531.1525, found 531.1583.

[0674] Based on the procedures of Examples 1 through 4 and using theappropriate amide forming amine, additional examples prepared aresummarized in Table 1. TABLE 1

Example Number Y 5

6

7

8

[0675] Schemes 3 and 4 below summarize generic procedures that permitthe preparation of a wide variety of the compounds of the presentinvention through the ability to introduce numerous R² substituents, awide variety of amino substituting

[0676] groups represented by B-A, and a large number of amide forming Ygroups at the carboxylic acid group in which K is an alkylene,methylene. Example 9 below shows the preparation of a compound whereinX⁰ and R¹ are each hydrido and J and R² are each fluoro.

Example 9

[0677]

[0678] 2,6-Difluorophenylacetic acid was added in small portions over aperiod of 20 minutes to fuming nitric acid chilled to −10° C.(methanol/ice). The addition was closely monitored to keep thetemperature below 5° C. Upon complete addition, the solution stirred at−10° C. for 15 minutes. The solution was poured over ice/water andextracted with ether. The organic layer was washed with brine, driedover magnesium sulfate, and filtered. The solvent was removed byevaporation to afford 5.75 g (91%) of a white solid of product EX-9A; ¹HNMR ppm: 3.89 (s, 2H), 7.11(m, 1H), 8.16 (m, 1H); ¹⁹F NMR ppm: −101.66(m, 1F), −115.43 (m, 1F).

[0679] Oxalyl chloride (12.6 mL, 0.144 mol) was added to a solution ofthe acid EX-9A (5.75 g, 0.026 mol) in dichloromethane followed by a dropof dimethyl formamide. After stirring at room temperature for 1 hour,the solvent was removed by evaporation to afford the acid chloride. Theacid chloride was redissolved into dichloromethane and an excess ofmethanol (50 mL) was added followed by addition of pyridine (3.5 mL,0.043 mol). The solution stirred at room temperature for 5 hours. Thesolution was washed with water, brine, and dried over magnesium sulfateand the solvent was removed by evaporation to afford the crude product.The product was purified by column chromatography (30% ethylacetate-hexane) to afford 5.47 g (91%) of an orange oil of productEX-9B; ¹H NMR ppm: 3.78 (s, 3H), 3.84 (s, 2H), 7.09 (m, 1H), 8.12 (m,1H); ¹⁹F NMR ppm: −101.76 (m, 1F), 115.58 (m, 1F); HPLC purity(retention time): >99% (2.88 min).

[0680] The nitro compound EX-9B (6.87 g, 0.029 mmol) was stirred inglacial acetic acid. Powdered iron (8.29 g, 0.148 mmol) was added andthe solution was heated to 80° C. with vigorous stirring. The solutionwas stirred at 80° C. for 15 minutes at which, point the iron had turnedgray. The reaction, mixture was filtered through celite and the solidwas washed with ether. The resultant organic layer was washed withwater, stirred with saturated sodium bicarbonate until basic, and washedwith water again. The solution was dried over magnesium sulfate,filtered and the solvent was removed to afford the crude product. Theproduct was purified by column chromatography (30% ethyl acetate-hexane)to afford 4.07 g (68%) of a clear oil of product EX-9C; ¹H NMR ppm: 3.62(bs, 2H), 3.71 (s, 2H), 3.74 (s, 3H), 6.70 (m, 2H); ¹⁹F NMR ppm: −115.58(m, 1F), −129.12 (m, 1F); HPLC purity (retention time): >99% (1.57 min).

[0681] Diisopropylethylamine (5.1 mL, 0.029 mol) was added to a solutionof the aniline EX-9C (4.0 g, 0.019 mmol) and a-toluenesulfonyl chloride(8.34 g, 0.042 mol) in dichioromethane, and the resulting solutionstirred at room temperature for 20 hours. The solution was washed with 2N hydrochloric acid, brine, dried over magnesium sulfate, and filtered.The solvent was removed by evaporation to afford the crude product. Theproduct was purified by column chromatography (30% ethyl acetate-hexane)to afford 6.2 g (61%) of a tan solid of product EX-9D; 1H NMR ppm: 3.73(s, 2H), 3.75 (s, 3H), 4.63 (d, 2H), 5.10 (d, 2H), 5.91 (m, 1H), 6.47(m, 1H), 7.45 (m, 1OH); ¹⁹F NMR ppm: −109.09 (m, 1F), −115.57 (m, 1F);,HPLC purity (retention time): 85.3% (4.45 min).

[0682] Aqueous sodium hydroxide (10%) (10.3 mL, 0.025 mol) was added toa solution of the methyl ester EX-9D (3.29 g, 0.0064 mol) in methanoland the resulting solution stirred at 65° C. for 4 hours. The solutionwas acidified with 2 N hydrochloric acid and extracted with ether. Thesolution was washed with brine, dried over magnesium sulfate, andfiltered. The solvent was removed by evaporation to afford 2.1 g (95%)of a white solid of product EX-9E; ¹H NMR ppm: 3.87 (s, 2H), 4.60 (s,2H), 7.11 (m, 1H), 7.51 (m, 6H), 9.77 (s, 1H); ¹⁹F NMR ppm: −119.10 (m,1F), −123.54 (m, 1F); HPLC purity (retention time): >99% (2.86 min);HRMS calcd for C₁₅H₁₃O₄N₁S₁F₂ (M⁺+NH₄) 359.0877, found 359.0867.

[0683] Reaction of EX-9E with N-Boc-piperidinylmethylamine afforded 67.2mg (125%) of a clear oil of product EX-9F; ¹H NMR ppm: 1.14 (m, 2H),1.47 (s, 9H), 1.65 (m, 3H), 2.69 (m, 2H), 3.18 (m, 2H), 3.62 (s, 2H),4.10 (m, 2H), 4.38 (s, 2H), 6.01 (m, 1H), 6.90 (m, 2H), 7.35 (m, 6H);¹⁹F NMR ppm: −117.94 (m, 1F), −126.43 (m, 1F); HPLC purity (retentiontime): 56.6% (3.57 min).

[0684] Deprotection of EX-9F using the procedures of Example 1 afforded40.6 mg (93%) of a white solid of product; ¹H NMR ppm: 1.04 (m, 2H),1.32 (m, 3H), 2.35 (m, 3H), 2.86 (m, 2H), 3.06 (s, 2H), 3.78 (s, 2H),6.26 (m, 1H), 6.74 (m, 6H), 7.57 (bs, 1H), 8.73 (m, 1H), 8.99 (m, 1H);¹⁹F NMR ppm: −118.93 (m, 1F), −123.81 (m, 1F); HPLC purity (retentiontime): 88.1% (2.36 min); HRMS calcd for C₂₁H₂₅O₃N₃S₁F₂ (M⁺+H) 438.1663,found 438.1642.

Example 10

[0685]

[0686] Using the procedure of Example 9 with 4-dimethylaminobenzylamineafforded 55.5 mg (117%) of a white solid of product; ¹H NMR ppm: 2.50(s, 6H), 3.26 (s, 2H), 3.89 (s, 2H), 3.93 (d, 2H), 6.27 (bd, 1H), 6.43(m, 1H), 6.72 (m, 2H), 6.93 (r, 6H), 7.44 (m, 1H), 7.58 (s, 1H), 8.84(s, 1H); ¹⁹F NMR ppm: −118.49 (m, 1F), −124.01 (m, 1F); HPLC purity(retention time): >99% (2.57 min); HRMS calcd for C₂₄H₂₅O₃N₃S₁F₂ (M⁺+H)474.1663, found 474.1647.

Example 11

[0687]

[0688] Using the procedure of Example 9 with pyridylmethylamine afforded51.2 mg (118%) of a white solid of product; ¹H NMR ppm: 3.21 (s, 2H),3.82 (s, 2H), 3.93 (d, 2H), 6.37 (m, 1H), 6.78 (m, 8H), 7.29 (s, 1H),7.46 (s, 1H), 8.91 (s, 1H); ¹⁹F NMR ppm: −118.95 (m, 1F), −123.95 (m,1F); HPLC purity (retention time): 91% (2.34 min); HRMS calcd forC₂₁H₁₉O₃N₃S₁F₂ (M⁺+H) 432.1193, found 432.1164.

Example 12

[0689]

[0690] Using the procedure of Example 9 with3-(imidazol-1-yl)propylamine afforded 55.5 mg (123%) of a clear oil ofproduct; ¹H NMR ppm: 1.97 (m, 2H), 3.24 (m, 2H), 3.58 (s, 2H), 3.94 (m,2H), 4.34 (s, 2H), 6.61 (m, 1H), 7.71 (m, 2H), 6.89 (m, 3H), 7.32 (m,7H), 8.02 (s, 1H); ¹⁹F NMR ppm: −118.56 (m, 1F), −125.29 (m, 1F); HPLCpurity (retention time): 51.0% (2.28 min); HRMS calcd for C₂₁H₂₂O₃N₄S₁F₂(M⁺+H) 449.1459, found 449.1455.

Example 13

[0691]

[0692] Using the procedures of Example 9 and the amine3-(N-Cbz-amidino)benzylamine afforded 37.7 mg (62%) of a clear oil ofproduct EX-13A; ¹H NMR ppm: 3.62 (m, 2H), 4.29 (s, 2H), 4.42 (d, 2H),5.12 (s, 2H), 6.80 (m, 2H), 7.38 (m, 14H), 7.71 (m, 2H); ¹⁹F NMR ppm:−117.61 (m, 1F), −125.19 (m, 1F); HPLC purity (retention time): 69.6%(3.25 mn).

[0693] The benzyloxycarbonyl (Cbz) compound EX-13A (0.010 mmol), sodiumiodide (60.0 mg, 0.040 mmol), and trimethylsilyl chloride (50.7 uL,0.040 mmol) were stirred in acetonitrile at 55° C. for 18 hours.Methanol (100 uL) was added and the solution stirred at room temperaturefor 2 hours. The dimethylbenzylamine resin (3.58 meq/g) (0.60 g, 2.1mmol) was added and the solution stirred at room temperature for 4hours. The reaction mixture was filtered through celite and the solidwas rinsed with acetonitrile. The combined filtrate and washings wereevaporated to afford 89.9 mg (71%) of a white solid of product; ¹H NMRppm: 3.00 (s, 2H), 3.62 (s, 2H), 3.76 (d, 2H), 6.12 (m, 1H), 6.58-7.32(m, 13H), 7.88 (m, 1H); ¹⁹F NMR ppm: −120.82 (m, 1F), −124.52 (m, 1F);HPLC purity (retention time): 66.4% (2.60 min); HRMS calcd forC₂₃H₂₂O₃N₄S₁F₂ (M⁺+H) 473.1459, found 473.1449.

Example 14

[0694]

[0695] Using the procedures of Example 9 and the amine,4-(N-Cbz-amidino)benzylamine, afforded 49.9 mg (82%) of a clear oil ofproduct EX-14A; ¹H NMR ppm: 3.58 (m, 2H), 4.27 (s, 2H), 4.32 (d, 2H),5.18 (s, 2H), 6.74 (m, 2H), 7.14 (d, 2H), 7.37 (m, 12H), 7.68 (d, 2H);¹⁹F NMR ppm: −117.58 (m, 1F), −124.63 (m, 1F); HPLC purity (retentiontime): 81.7% (3.14 min).

[0696] Using the procedure of Example 13, EX-14A afforded 89.9 mg (71%)of a white solid of product x; ¹H NMR ppm: 3.21 (s, 2H), 3.94 (s, 2H),4.06 (m, 2H), 5.94 (bs, 1H), 6.42 (m, 1H), 6.91 (m, 8H), 7.12 (d, 2H),7.49 (d, 2H), 8.18(m, 1H); ¹⁹F NMR ppm: −119.65 (m, 1F), −124.41 (m,1F); HPLC purity (retention time): 44.1% (2.57 min); HRMS calcd forC₂₃H₂₂O₃N₄S₁F₂ (M⁺+H) 473.1459, found 473.1447.

Example 15

[0697]

[0698] Using the procedures of Example 9 and the amine,5-(N,N-bis-Boc-guanidino)pentylamine, afforded 67.1 mg (100%) of a clearoil of product EX-15A; ¹H NMR ppm: 1.57 (m, 18H), 1.58 (m, 6H), 3.26 (m,2H), 3.40 (m, 2H), 3.60 (s, 2H), 4.35 (s, 2H), 6.10 (m, 1H), 6.86 (m,1H), 7.37 (m, 8H), 8.31 (m, 1H); ¹⁹F NMR ppm: −117.86 (m, 1F), −125.96(m, 1F); HPLC purity (retention time): 39.2% (3.48 min).

[0699] Reaction of EX-15A using the procedure of Example 1 fordeprotection afforded 41.2 mg (88%) of a white solid of product; ¹H NMRppm: 0.83 (m, 6H), 2.71 (m, 2H), 3.05 (s, 2H), 3.16 (m, 2H), 3.68 (s,2H), 6.25 (m, 1H), 6.74 (m, 8H); HPLC purity (retention time): >99%(2.66 min); HRMS calcd for C₂₁H₂₇O₃N₅S₁F₂ (M⁺+H) 468.1881, found468.1842.

[0700] Scheme 5 below summarizes a generic procedure that permits thepreparation of a wide variety of the compounds of the present inventionthrough the ability to introduce numerous R² substituents, a widevariety of amino substituting groups represented by B-A, and a largenumber of amide forming Y groups at the carboxylic acid group in which Kis an alkylene, methylene. Example 16 below shows the preparation of acompound wherein X⁰ and R¹ are each hydrido and J and R² are eachfluoro.

Example 16

[0701]

[0702] Sodium triacetoxyborohydride (7.2 g, 0.033 mol) was added to asolution of the methyl 3-amino-2,6-difluorophenylacetate (1.72 g, 0.0085mol), phenylacetaldehyde (2.0 mL, 0.015 mol), and a drop of acetic acidin a tetrahydrofuran-dichloromethane (1:1) solution. After stirring atroom temperature for 18 hours, sodium hydroxide (1N) was added untilbasic. The solution was extracted with dichloromethane and the organiclayer was washed with brine, dried over magnesium sulfate, and filtered.The solvent was removed by evaporation to afford a mixture of twoproducts. Fraction one of column chromatography (10% ethylacetate-hexane) afforded 1.25 g (36%) of a clear oil of theN,N-bis-phenylethyl; ¹H NMR ppm: 2.79 (t, 4H), 3.40 (t, 4H), 3.79 (s,5H), 6.87 (m, 2H), 7.25 (m, 10H); ¹⁹F NMR ppm: −122.50 (m, 1F), −123.67(m, 1F); HPLC purity (retention time): 95.7% (4.71 min); HRMS calcd forC₂₅H₂₅O₂N₁F₂ (M⁺+H) 410.1932, found 410.1926. Fraction two of the columnchromatography (10% ethyl acetate-hexane) afforded 1.06 g (41%) of aclear oil of product EX-16A; ¹H NMR ppm: 2.97 (t, 2H), 3.42 (t, 2H),3.73 (s, 2H), 3.75 (s, 3H), 6.62 (m, 1H), 6.82 (m, 1H), 7.29 (m, 5H);¹⁹F NMR ppm: −131.28 (m, 1F), −137.00 (m, 1F); HPLC purity (retentiontime): 96.1% (3.93 min); HRMS calcd for C₁₇H₁₇O₂N₁F₂ (M⁺+H) 306.1306,found 306.1309.

[0703] Aqueous sodium hydroxide (10%) (5.5 mL, 13.7 mmol) was added to asolution of the methyl ester Ex-16A (1.06 g, 3.47 mmol) in methanol andthe resulting solution stirred at 60° C. for 1 hour. The solution wasacidified with 2 N hydrochloric acid and extracted with ether. Thesolution was washed with brine, dried over magnesium sulfate, andfiltered. The solvent was removed by evaporation to afford 0.93 g (92%)of a white solid of product EX-16B; ¹H NMR ppm: 2.64 (t, 2H), 3.02 (t,2H), 3.19 (s, 2H), 6.46 (m, 1H), 6.75 (m, 6H), 7.10 (bd, 1H), 9.30 (bs,1H); ¹⁹F NMR ppm: −119.37 (m, 1F), −128.26 (m, 1F); HPLC purity(retention time): >99% (3.26 min); HRMS calcd for C₁₆H₁₅O₂N₁F₂ (M⁺+H)292.1149, found 292.1150.

[0704] 1-Hydroxybenzotriazole (43.1 mg, 0.31 mmol) was added to a slurryof the acid EX-16B (0.93 g, 3.19 mmol) and PS-carbodiimide (PSDCC) (1.00mmol/g) (9.57 g, 9.57 mmol) in a dichloromethane-dimethylformamide (3:1)solution. The suspension was agitated for 15 minutes. The amine,4-(N-Cbz-amidino)benzylamine (0.96 g, 3.16 mmol) and N-methylmorpholine(2.0 mL, 18.1 mmol) was added and the suspension was agitated for 2hours. Upon completion of the reaction, the polyamine resin (PSA) (2.69mmol/g) (1.0 g, 2.69 mmol) and polymer-bound aldehyde (PSCHO) (2.3mmol/g) (0.50 g, 1.15 mmol) was added and the suspension was agitatedfor 1 hour. The solution was filtered and the polymers were rinsed withdimethylformamide and dichloromethane until no more UV activity was seenin the dichloromethane washing. The combined filtrate and washings wereevaporated to afford the product. The product was purified by columnchromatography (70% ethyl acetate-hexane) to afford 1.14 g (64%) of awhite solid of product EX-16C; ¹H NMR ppm: 2.92 (t, 2H), 3.37 (m, 2H),3.64 (s, 2H), 3.86 (bs, 1H), 4.39 (d, 2H), 5.23 (s, 2H), 6.41 (m, 1H),6.57 (m, 1H), 6.79 (m, 1H), 7.34 (m, 14H), 7.72 (d, 2H), 9.43 (bs, 1H);¹⁹F NMR ppm: −131.01 (m, 1F), −136.68 (m, 1F); HPLC purity (retentiontime): 83.6% (3.38 min); HRMS calcd for C₃₂H₃₀O₃N₄F₂ (M⁺+H) 557.2364,found 557.2326.

[0705] Reaction of EX-16C according to Example 13 afforded 0.58 g (82%)of a yellow oil of product; ¹H NMR ppm: 3.16 (t, 2H), 3.72 (m, 2H), 3.86(s, 2H), 4.66 (s, 2H), 7.32 (m, 7H), 7.68 (m, 3H), 7.82 (d, 2H), 8.78(bs, 1H), 9.27 (bs, 1H); ¹⁹F NMR ppm: −112.97 (m, 1F), −125.49 (m, 1F);HPLC purity (retention time): 63.3% (2.77 min); HRMS calcd forC₂₄H₂₄O₁N₄F₂ (M⁺+H) 423.1996, found 423.1953.

[0706] Schemes 6 and 7 below summarize a generic procedure that permitsthe preparation of a wide variety of the compounds of the presentinvention through the ability to introduce numerous Q (R², wherein Z⁰ isa covalent bond) aryl and heteroaryl substituents, a wide variety ofamino substituting groups represented by B-A, and a large number ofamide forming Y groups at the carboxylic acid group in which K is analkylene, methylene. Example 17 below shows the preparation of acompound wherein X⁰ and R¹ are each hydrido, J is fluoro, Z⁰ is acovalent bond, and Q is the substituent, phenyl.

Example 17

[0707]

[0708] The nitro compound methyl 3-nitro-2,6-difluorophenylacetate (18.3g, 0.079 mol) was added to a solution of trimethylacetic acid (24.3 g,0.23 mol) and potassium carbonate (54.5 g, 0.39 mol) indimethylsulfoxide and the resulting solution stirred at 80° C. for 15minutes. The reaction was diluted with water and diethyl ether and theresulting solution was acidified with 2 N hydrochloric acid andextracted with ether. The solution was washed with brine, dried overmagnesium sulfate, and filtered. The solvent was removed by evaporationto afford a mixture of two products. Fraction one of columnchromatography (40% ethyl acetate-hexane) afforded 12.1 g (67%) of ayellow solid of product methyl 3-nitro-2-hydroxy-6-fluorophenylacetate;¹H NMR ppm: 3.71 (s, 3H), 3.81 (s, 2H), 6.80 (m, 1H), 8.18 (m, 1H); ¹⁹FNMR ppm: −99.71 (m, 1F); HPLC purity (retention time): >99% (2.63 min).Fraction two of column chromatography (40% ethyl acetate-hexane)afforded 4.97 g (27%) of a yellow solid of product EX-17A; ¹H NMR ppm:3.71 (s, 3H), 3.80 (d, 2H, J_(HF)=1.7 Hz), 6.95 (dd, 1H, , J_(HH)=9.2Hz, J_(HF)=1.1 Hz), 8.05 (m, 1H); ¹⁹F NMR ppm: −120.02 (d, 1F,J_(HF)=8.7 Hz); HPLC purity (retention time): >99% (2.25 min).

[0709] Triethylamine (729 uL, 5.2 mmol) was added to a solution of thephenol EX-17A (1.0 g, 4.36 mmol) and triflic anhydride (807 uL, 4.7mmol) in dichloromethane at −10° C. After stirring at room temperaturefor 18 hours, the solution was acidified with hydrochloric acid 2N andextracted with dichloromethane. The organic layer was washed with brine,dried over magnesium sulfate, and filtered. The solvent was removed byevaporation to afford the crude product. The product was purified bycolumn chromatography (20% ethyl acetate-hexane) to afford 1.0 g (68%)of a clear oil of product EX-17B; ¹H NMR ppm: 3.79 (s, 3H), 3.90 (d, 2H,J_(HF)=2.0 Hz), 7.38 (dd, 1H, J_(HH)=7.6 Hz, J_(HF)=1.8 Hz), 8.18 (m,1H); 1⁹F NMR ppm: −73.61 (s, 3F), −113.78 (m, 1F); HPLC purity(retention time): 94.6% (3.69 min).

[0710] The triflate compound EX-17B (1.0 g, 2.76 mmol) was added to asolution of tri-n-butylphenylstannane (1.0 mL, 3.0 mmol), lithiumchloride (351 mg, 8.28 mmol), andtetrakis(triphenylphosphine)palladium(O) (63.9 mg, 0.055 mmol) in 14 mLof anhydrous dioxane. The solution was heated to 85° C. for 4 hours andthen at room temperature for 12 hours. The organic layer was washed withbrine, dried over magnesium sulfate, and filtered. The solvent wasremoved by evaporation to afford the crude product. The product waspurified by column chromatography (20% ethyl acetate-hexane) to afford0.62 g (78%) of a yellow oil of product EX-17C; ¹H NMR ppm: 3.73 (s,5H), 7.28 (m, 3H), 7.49 (m, 3H), 8.07 (m, 1H); ¹⁹F NMR ppm: −118.75 (m,1F); HPLC purity (retention time): >99% (3.81 min).

[0711] The nitro compound EX-17C (0.60 g, 2.0 mmol) was stirred inglacial acetic acid. Powdered iron (0.60 g, 10.7 mmol) was added and thesolution was heated to 70° C. with vigorous stirring. The solution wasstirred at 70° C. for 30 minutes at which point the iron had turnedgray. The reaction mixture was filtered through celite and the solid waswashed with ether. The resultant organic layer was washed with water,brine, dried over magnesium sulfate, and filtered. The solvent wasremoved by evaporation to afford 0.47 g (91%) of a clear oil of productEX-17D; ¹H NMR ppm: 3.64 (d, 2H, J_(HF)=2.3 Hz), 3.71 (s, 3H), 6.83 (m,1H), 7.27 (dd, 1H), 7.37 (m, 5H); ¹⁹F NMR ppm: −137.27 (d, 1F,J_(HF)=8.7 Hz); HPLC purity (retention time): 93.2% (2.76 min); HRMScalcd for C₁₅H₁₄O₂N₁F₁ (M⁺+NH₄) 277.1352, found 277.1337.

[0712] Sodium triacetoxyborohydride (1.7 g, 8.0 mmol) was added to asolution of the aniline EX-17D (0.051 g, 2.0 mmol), phenylacetaldehyde(281 uL, 0.015 mol), and a drop of acetic acid in atetrahydrofuran-dichloromethane (1:1) solution. After stirring at roomtemperature for 5 hours, the solution was diluted with ether and water.The organic layer was washed with brine, dried over magnesium sulfate,and filtered. The solvent was removed by evaporation to afford 0.58 g(80%) of a yellow oil of product EX-17E; ¹H NMR ppm: 3.02 (t, 2H), 3.51(m, 2H), 3.64 (d, 2H, J_(HF)=2.9 Hz), 3.70 (s, 3H), 6.80 (m, 1H), 7.02(dd, 1H), 7.31 (m, 10H); ¹⁹F NMR ppm: −138.50 (d, 1F); HPLC purity(retention time): 83.2% (4.69 min); HRMS calcd for C₂₃H₂₂O₂N₁F₁ (M⁺+H)364.1713, found 364.1703.

[0713] Aqueous sodium hydroxide (10%) (2.5 mL, 6.2 mmol) was added to asolution of the methyl ester EX-17E (0.58 g, 1.6 mmol) in methanol andthe resulting solution stirred at 65° C. for 5 hours. The solution wasacidified with 2 N hydrochloric acid and extracted with diethyl ether.The solution was washed with brine, dried over magnesium sulfate, andfiltered. The solvent was removed by evaporation to afford 0.47 g (84%)of an orange glass of product EX-17F; 1H NMR ppm: 3.02 (t, 2H), 3.51 (m,2H), 3.68 (d, 2H, J_(HF)=2.6 Hz), 6.84 (m, 1H), 7.04 (dd, 1H), 7.31 (m,10H); ¹⁹F NMR ppm: −137.47 (d, 1F); HPLC purity (retention time): >99%(4.08 min); HRMS calcd for C₂₂H₂₀02N₁F₁ (M⁺+H) 350.1556, found 350.1532.

[0714] 1-Hydroxybenzotriazole (180 mg, 1.3 mmol) was added to a slurryof the acid EX-17F (0.47 g, 1.34 mmol) and PS-carbodiimide (1.00 mmol/g)(2.6 g, 2.6 mmol) in a dichloromethane-dimethylformamide (3:1) solution.The suspension was agitated for 15 minutes. The amine4-(N-Cbz-amidino)benzylamine (0.51 g, 1.6 mmol) and N-methylmorpholine(295 uL, 2.6 mmol) was added and the suspension was agitated for 2hours. Upon completion of the reaction, the polyamine resin (PSA) (2.81mmol/g) (1.0 g, 2.81 mmol) and polymer-bound aldehyde (PSCHO) (2.3mmol/g) (1.0 g, 2.30 mmol) were added and the suspension was agitatedfor 1 hour. The solution was filtered and the polymer was rinsed withdimethylformamide and dichloromethane until no more UV activity was seenin the dichloromethane washing. The combined filtrate and washings wereevaporated to afford the product. The product was purified by columnchromatography (60% ethyl acetate-hexane) to afford 0.79 g (96%) of awhite solid of product EX-17G; ¹H NMR ppm: 2.92 (m, 2H), 3.19 (m, 2H),3.77 (d, 2H), 4.67 (d, 2H), 5.40 (s, 2H), 5.60 (bm, 1H), 7.08 (m, 1H),7.15 (dd, JH), 7.54 (m, 16H), 8.28 (m, 3H), 8.59 (bt, 1H), 9.40 (bs,1H), 9.65 (bs, 1H); ¹⁹F NMR ppm: 138.15 (d, 1F); HPLC purity (retentiontime): >99% (4.00 min); HRMS calcd for C₂₂H₂₀O₂N₁F₁ (M⁺+H) 615.2771,found 615.2760.

[0715] A catalytic amount of palladium on carbon (10%) in dioxane wasadded to a methanol-4N hydrochloric acid/dioxane (3:1) solution of theCbz compound EX-17G (200 mg, 0.32 mmol) and the mixture was stirredunder a balloon of hydrogen at room temperature for 12 hours. Themixture was filtered through celite and the solvent was evaporated toafford the product. The product was purified by reverse-phasechromatography to afford 142 mg (92%) of a white solid of product; ¹HNMR ppm: 2.97 (t, 2H), 3.48 (t, 2H), 3.61 (d, 2H), 4.64 (d, 2H), 6.80(m, 1H), 6.97 (dd, 1H), 7.33 (m, 11H), 7.47 (d, 2H), 7.79 (d, 2H); ¹⁹FNMR ppm: −77.60 (s, 6F), −139.78 (d, 1F); HPLC purity (retentiontime): >99% (3.22 min).

[0716] Schemes 8 and 9 below summarize a generic procedure that permitsthe preparation of a wide variety of the compounds of the presentinvention through the ability to introduce numerous Q (R², wherein Z⁰ isa covalent bond) aryl and heteroaryl substituents, a wide variety ofamino substituting groups represented by B-A, and a large number ofamide forming Y groups at the carboxylic acid group in which K is analkylene, methylene. Example 18 below shows the preparation of acompound wherein X⁰ and R¹ are each hydrido, J is methoxy, Z⁰ is acovalent bond, and Q is the substituent, phenyl.

Example 18

[0717]

[0718] Iodomethane (20.0 mL, 0.32 mol) was added to a solution of thephenol, methyl, 2-hydroxy-3-nitro-6-fluorophenylacetate, (5.0 g, 0.022mol) and potassium carbonate (9.0 g, 0.065 mol) in tetrahydrofuran.After stirring at 65° C. for 18 hours, the was diluted with waterextracted with diethyl ether. The organic layer was washed with brine,dried over magnesium sulfate, and filtered. The solvent was removed byevaporation to afford the crude product. The product was purified bycolumn chromatography (15% ethyl acetate-hexane) to afford 4.18 g (79%)of a yellow oil of product EX-18A; ¹H NMR ppm: 3.76 (s, 3H), 3.70 (d,2H, J_(HF)=1.5 Hz), 3.93 (s, 3H), 7.00 (m, 1H), 7.94 (m, 1H); ¹⁹F NMRppm: −103.51 (m, 1F); HPLC purity (retention time): >99% (2.60 min).

[0719] Aqueous sodium hydroxide (10%) (25 mL, 0.062 mol) was added to asolution of the fluoro compound EX-18A (4.0 g, 0.016 mol) intetrahydrofuran and the resulting solution stirred at 90° C. for 14hours. The solution was acidified with 4 N hydrochloric acid andextracted with ether. The solution was washed with brine, dried overmagnesium sulfate, and filtered. The solvent was removed by evaporationto afford the crude product in which fluorine NMR revealed no signal.The product was dissolved into dichloromethane and oxalyl chloride (7.0mL, 0.080 mol) was added to the solution followed by a drop ofdimethylformamide. After stirring at room temperature for 1.5 hours, thesolvent was removed by evaporation to afford the acid chloride. The acidchloride was redissolved into dichloromethane and an excess of methanol(50 mL) was added followed by addition of pyridine (2.6 mL, 0.032 mol).The solution stirred at room temperature for 5 hours. The solution waswashed with water, brine, dried over magnesium sulfate, and filtered.The solvent was removed by evaporation to afford a mixture of twoproducts. Fraction one of column chromatography (25% ethylacetate-hexane) afforded 2.0 g (49%) of a yellow solid of product methyl2,6-dimethoxy-3-nitrophenylacetate; ¹H NMR ppm: 3.73 (s, 3H), 3.76 (s,2H), 3.90 (s, 3H), 3.93 (s, 3H), 6.75 (d, 1H, J=9.3 Hz), 8.03 (d, 1H,J=9.3 Hz); HPLC purity (retention time): >99% (2.64 min). Fraction twoof column chromatography (25% ethyl acetate-bexane) afforded 1.33 g(34%) of a white solid of phenol product EX-18B; ¹H NMR ppm: 3.84 (s,3H), 3.85 (s, 2H), 3.94 (s, 3H), 6.78 (d, 1H, J=8.9 Hz), 7.90 (d, 1H,J=8.9 Hz), 8.19 (s, 1H); HPLC purity (retention time): >99% (2.14 min).

[0720] Triethylamine (910 uL, 6.5 mmol) was added to a solution of thephenol EX-18B (1.3 g, 5.5 mmol) and triflic anhydride (1.0 mL, 5.9 mmol)in dichloromethane at −10° C. After stirring at room temperature for 18hours, the solution was acidified with hydrochloric acid 2N andextracted with dichloromethane. The organic layer was washed with brine,dried over magnesium sulfate, and filtered. The solvent was removed byevaporation to afford the crude product. The product was purified bycolumn chromatography (15% ethyl acetate-hexane) to afford 1.7 g (83%)of a clear oil of product EX-18C; ¹H NMR ppm: 3.78 (s, 3H), 3.87 (d,2H), 3.96 (s, 3H), 7.27 (d, 1H, J=9.2 Hz), 7.95 (d, 1H, J=9.2 Hz); ¹⁹FNMR ppm: −73.89 (s, 3F); HPLC purity (retention time): >99% (3.62 min).

[0721] The triflate compound EX-18C (1.7 g, 4.5 mmol) was added to asolution of tri-n-butylphenylstannane (1.8 mL, 5.5 mmol), lithiumchloride (580 mg, 13.6 mmol), andtetrakis(triphenylphosphine)palladium(O) (11.0 mg, 0.095 mmol) in 23 mLof anhydrous dioxane. The solution was heated to 85° C. for 18 hours.The organic layer was washed with brine, dried over magnesium sulfate,and filtered. The solvent was removed by evaporation to afford the crudeproduct. The product was purified by column chromatography (15% ethylacetate-hexane) to afford 1.0 g (73%) of a white solid of productEX-18D; ¹H NMR ppm: 3.69 (s, 5H), 3.94 (s, 3H), 7.17 (d, 1H, J=8.3 Hz),7.29 (m, 2H), 7.45 (m, 3H), 7.89 (d, 1H, J=8.3 Hz); HPLC purity(retention time): >99% (3.60 min).

[0722] The nitro compound EX-18D (1.0 g, 3.3 mmol) was stirred inglacial acetic acid. Powdered iron (0.92 g, 16.4 mmol) was added and thesolution was heated to 80° C. with vigorous stirring. The solution wasstirred at 80° C. for 15 minutes at which point the iron had turnedgray. The reaction mixture was filtered through celite and the solid waswashed with ether. The resultant organic layer was washed with water,brine, dried over magnesium sulfate, and filtered. The solvent wasremoved to afford the product EX-18E. The product was not purified andcarried on to the next step. HPLC purity (retention time): >99% (2.48min).

[0723] Sodium triacetoxyborohydride (2.8 g, 13.2 mmol) was added to asolution of the aniline EX-18E (0.89 g, 3.3 mmol), phenylacetaldehyde(540 uL, 39.2 mmol), and a drop of acetic acid in atetrahydrofuran-dichloromethane (1:1) solution. After stirring at roomtemperature for 2 hours, the solution was diluted with dichloromethaneand water. The organic layer was washed with brine, dried over magnesiumsulfate, and filtered. The solvent was removed by evaporation to affordthe crude product. The product was purified by column chromatography(25% ethyl acetate-hexane) to afford 0.69 g (56%) of a yellow oil ofproduct EX-18F; ¹H NMR ppm: 3.04 (t, 2H), 3.50 (t, 2H), 3.69 (s, 3H),3.67 (s, 2H), 3.69 (s, 3H), 6.75 (d, 1H, J=8.3 Hz), 7.02 (d, 1H, J=8.3Hz), 7.35 (m, 10H); HPLC purity (retention time): >99% (4.37 min).

[0724] Aqueous sodium hydroxide (10%) (2.9 mL, 7.2 mmol) was added to asolution of the methyl ester EX-18F (0.69 g, 1.8 mmol) in methanol andthe resulting solution stirred at 60° C. for 5 hours. The solution wasacidified with 2 N hydrochloric acid and extracted with diethyl ether.The solution was washed with brine, dried over magnesium sulfate, andfiltered. The solvent was removed by evaporation to afford 0.66 g (100%)of an orange foam of product EX-18G; HPLC purity (retention time): 80%(3.83 min).

[0725] 1-Hydroxybenzotriazole (247 mg, 1.8 mmol) was added to a slurryof the acid EX-18G (0.66 g, 1.83 mmol) and PS-carbodiimide (PSDCC) (1.00mmol/g) (3.6 g, 3.6 mmol) in a dichloromethane-dimethylformamide (3:1)solution. The suspension was agitated for 15 minutes. The amine,4-(N-Cbz-amidino)benzylamine, (0.70 g, 2.2 mmol) and N-methylmorpholine(1.0 mL, 9.0 mmol) was added and the suspension was agitated for 18hours. Upon completion of the reaction, the polyamine resin (PSA) (2.81mmol/g) (1.0 g, 2.81 mmol) and polymer-bound aldehyde (PSCHO) (2.3mmol/g) (1.0 g, 2.30 mmol) were added and the suspension was agitatedfor 1 hour. The solution was filtered and the polymer was rinsed withdimethylformamide and dichloromethane until no more UV activity was seenin the dichloromethane washing. The combined filtrate and washings wereevaporated to afford the product. The product was purified by columnchromatography (60% ethyl acetate-hexane) to afford 0.52 g (45%) of awhite solid of product EX-18H; ¹H NMR ppm: 3.17 (m, 2H), 3.65 (m, 2H),3.77 (s, 2H), 3.86 (s, 3H), 4.64 (d, 2H), 5.27 (bt, 1H), 4.40 (s, 2H),6.96 (d, 1H), 7.11 (d, 1H), 7.56 (m, 16H), 8.23 (m, 3H), 8.41 (bt, 1H),9.40 (bs, 1H), 9.75 (bs, 1H); HPLC purity (retention time): >99% (3.80min).

[0726] A catalytic amount of palladium on carbon (5%) in dioxane wasadded to 3 mL of a methanol-4N hydrochloric acid/dioxane (3:1) solutionof the Cbz compound EX-18H (22.8 mg, 0.036 mmol) and the mixture wasstirred under a balloon of hydrogen at room temperature for 12 hours.The mixture was filtered through celite and the solvent was evaporatedto afford the product. The product was purified by reverse-phasechromatography to afford 14.6 mg (81%) of a white solid of product x; ¹HNMR ppm: 3.00 (t, 2H), 3.50 (t, 2H), 3.63 (s, 2H), 3.67 (s, 3H), 4.41(s, 2H), 6.86 (m, 1H), 6.96 (m, 1H), 7.35 (m, 10H), 7.46 (d, 2H), 7.77(d, 2H), 8.21 (bs, 1H); HPLC purity (retention time): >99% (3.29 min).

[0727] Scheme 10 below summarizes a generic procedure that permits thepreparation of a wide variety of the phenolic compounds of the presentinvention through the ability to introduce numerous Q (R², wherein Z⁰ isa covalent bond) aryl and heteroaryl substituents, a wide variety ofamino substituting groups represented by B-A, and a large number ofamide forming Y groups at the carboxylic acid group in which K is analkylene, methylene. Example 19 below shows the preparation of acompound wherein X⁰ and R¹ are each hydrido, J is hydroxy, Z⁰ is acovalent bond, and Q is the substituent, phenyl.

Example 19

[0728]

[0729] The benzyloxycarbonyl (Cbz) compound from Example 18 (0.10 g,0.16 mmol), sodium iodide (0.19 g, 1.2 mmol), and trimethylsilylchloride (162 uL, 1.2 mmol) were stirred in acetonitrile at 55° C. for18 hours. Methanol (100 uL) was added and the solution stirred at roomtemperature for 1 hour. The dimethylbenzylamine resin (3.58 meq/g) (0.60g, 2.1 mmol) was added and the solution stirred at room temperature for1 hour. The reaction mixture was filtered through celite and the solidwas rinsed with acetonitrile. The combined filtrate and washings wereevaporated to afford a mixture of two products. Fraction one ofreverse-phase chromatography afforded 4.5 mg (4%) of a white solid ofproduct; ¹H NMR ppm: 3.12 (t, 2H), 3.66 (m, 4H), 4.51 (s, 2H), 6.96 (d,1H), 7.36 (m, 12H), 7.55 (d, 2H), 7.80 (d, 2H); HPLC purity (retentiontime): 92% (2.53 min). Fraction two of reverse-phase chromatographyafforded 17.7 mg (32%) of a white solid of by-product,2,3-dihydro-2-oxo-3-phenyl-6-(N-(2-phenylethyl)amino-benzofuran, havingthe properties of ¹H NMR ppm: 3.06 (t, 2H), 3.63 (t, 2H), 3.88 (s, 2H),7.09 (d, 1H), 7.39 (m, 11H); HPLC purity (retention time): >99% (4.33min).

[0730] Schemes 11, 12, and 13 below summarize a generic procedure thatpermits the preparation of a wide variety of the substituted phenylcompounds of the present invention through the ability to introducenumerous Q (R², wherein Z⁰ is a covalent bond) aryl and heteroarylsubstituents, a wide variety of amino substituting groups represented byB-A, and a large number of amide forming Y⁰ groups at the carboxylicacid group in which K is an alkylene, such as methylene. Example 20below shows the preparation of a compound wherein X⁰ and R¹ are eachhydrido, J is fluoro, Z⁰ is a covalent bond, and Q is the substituent,3-aminophenyl.

Example 20

[0731]

[0732] Triethylamine (15.3 mL, 0.109 mol) was added to a solution of them-bromoaniline (10.0 mL, 0.092 mol) and benzylchloroformate (13.7 mL,0.092 mol) in dichloromethane at 0° C. After stirring at roomtemperature for 2 hours, the solution was acidified with hydrochloricacid 2N and extracted with dichloromethane. The organic layer was washedwith brine, dried over magnesium sulfate, and filtered. The solvent wasremoved by evaporation to afford the crude product. The product waspurified by column chromatography (10% ethyl acetate-hexane) to afford14.8 g (53%) of a clear oil of product EX-20A; ¹H NMR ppm: 5.23 (s, 2H),6.80 (bs, 1H), 7.29 (m, 9H); HPLC purity (retention time): >99% (4.05min).

[0733] The bromo compound EX-20A (1.72 g, 5.6 mmol) was added to asolution of bis(tributyltin) (8.5 mL, 16.0 mmol), andtetrakis(triphenylphosphine)-palladium(0) (64.7 mg, 0.056 mmol) in 15 mLof toluene. The solution was heated to 90° C. for 18 hours. The solutionwas diluted with diethyl ether and the organic layer was washed with asaturated solution of potassium fluoride, brine, dried over magnesiumsulfate, and filtered. The solvent was removed by evaporation to affordthe crude product. The product was purified by column chromatography(10% ethyl acetate-hexane) to afford 1.36 g (47%) of a brown oil ofproduct EX-20B; ¹H NMR ppm: 0.90 (t, 9H), 1.04 (t, 6H), 1.33 (m, 6H),1.53 (m, 6H), 5.20 (s, 2H), 6.63 (bs, 1H), 7.37 (m, 9H).

[0734] The triflate compound EX-20B (1.31 g, 3.6 mmol) was added to asolution of the tin compound (2.17 mL, 4.2 mmol), lithium chloride (440mg, 10.0 mmol), and tetrakis(triphenylphosphine)palladium(0) (80.8 mg,0.070 mmol) in 18 mL of anhydrous dioxane. The solution was heated to85° C. for 21 hours. The organic layer was washed with brine, dried overmagnesium sulfate, and filtered. The solvent was removed by evaporationto afford the crude product. The product was purified by columnchromatography (40% ethyl acetate-hexane) to afford 0.56 g (38%) of ayellow oil of product EX-20C; ¹H NMR ppm: 3.64 (d, 2H), 3.70 (s, 3H),5.23 (s, 2H), 6.90 (m, 4H), 7.40 (m, 8H); ¹⁹F NMR ppm: −136.68 (d, 1F);HPLC purity (retention time): >99% (3.50 min).

[0735] Sodium triacetoxyborohydride (1.12 g, 5.28 mmol) was added to asolution of the aniline EX-20C (0.54 g, 1.32 mmol), benzaldehyde (147.8uL, 1.45 mmol), and a drop of acetic acid in atetrahydrofuran-dichloromethane (1:1) solution. After stirring at roomtemperature for 6 days, the solution was diluted with ether and water.The organic layer was washed with brine, dried over magnesium sulfate,and filtered. The solvent was removed by evaporation to afford the crudeproduct. The product was purified by column chromatography (20% ethylacetate-hexane) to afford 0.44 g (67%) of a yellow oil of productEX-20D; ¹H NMR ppm: 3.65 (d, 2H), 3.71 (s, 3H), 4.44 (s, 2H), 5.23 (s,2H), 6.72 (m, 2H), 6.97 (m, 2H), 7.36 (m, 8H); ¹⁹F NMR ppm: −138.06 (d,1F); HPLC purity (retention time): >99% (4.58 min).

[0736] Aqueous sodium hydroxide (10%) (1.4 mL, 3.5 mmol) was added to asolution of the methyl ester EX-20D (0.44 g, 0.88 mmol) in methanol andthe resulting solution stirred at 60° C. for 5 hours. The solution wasacidified with 2 N hydrochloric acid and extracted with diethyl ether.The solution was washed with brine, dried over magnesium sulfate, andfiltered. The solvent was removed by evaporation to afford 0.29 g (100%)of a white solid of two products EX-20E-1 and EX-20E-2. The productswere carried on to the next step.

[0737] PS-carbodiimide (PSDCC) (1.00 mmol/g) (1.4 g, 1.4 mmol) was addedto a slurry of the acids EX-20E-1 and EX-20E-2 (0.29 g, 0.71 mmole),1-hydroxybenzotriazole (95.9 mg, 0.71 mmol), amine (0.27 g, 0.84 mmol),and N-methylmorpholine (624 uL, 5.6 mmol) in adichloromethane-dimethylformamide (3:1) solution and the suspension wasagitated for 3 hours. Upon completion of the reaction, the polyamineresin (PSA) (2.81 mmol/g) (2.0 g, 5.6 mmol) and polymer-bound aldehyde(PSCHO) (2.3 mmol/g) (1.0 g, 2.30 mmol) were added and the suspensionwas agitated for 1 hour. The solution was filtered and the polymer wasrinsed with dimethylformamide and dichloromethane until no more UVactivity was seen in the dichloromethane washing. The combined filtrateand washings were evaporated to afford a mixture of two products.Fraction one of reverse-phase chromatography afforded 240 mg (50%) of ayellow solid of product EX-20F; ¹H NMR ppm: 3.60 (s, 3H), 3.69 (d, 2H),4.09 (s, 2H), 4.33 (s, 2H), 5.26 (s, 2H), 6.60-7.68 (m, 23H); ¹⁹F NMRppm: −138.00 (d, 1F); HPLC purity (retention time): 76% (3.71 min).

[0738] Fraction two of reverse-phase chromatography for EX-20F afforded180 mg (34%) of an orange oil of product EX-20G; ¹H NMR ppm: 3.68 (m,4H), 4.34 (s, 2H), 5.08 (s, 2H), 5.26 (s, 2H), 6.68-7.60 (m, 28H); ¹⁹FNMR ppm: −136.67 (bs, 1F); HPLC purity (retention time): 61% (4.15 min).

[0739] Hydrogen bromide in acetic acid (30% wt) was added to thecarbamate EX-20F or EX-20G and the solution stirred at room temperaturefor 16 hours. The solution was evaporated to afford a mixture of twoproducts. Fraction one of reverse-phase chromatography afforded 32 mg(52%) of an orange solid of the trihydrogen bromide product; ¹H NMR ppm:3.64 (s, 3H), 4.36 (d, 2H), 4.45 (s, 2H), 6.64 (m, 1H), 6.84 (dd, 1H),7.37 (m, 13H), 7.67 (d, 2H), 7.90 (bs, 2H), 8.97 (bs, 2H); ¹⁹F NMR ppm:−76.96 (s, 9F), −138.72 (d, 1F); HPLC purity (retention time): >99%(2.62 min).

[0740] Examples 21 and 22 summarize additional compounds prepared usingSchemes 11, 12, and 13.

Example 21

[0741]

[0742] The triflate compound, methyl2-fluoro-3-nitro-6-trifluoromethyl-sulfonyloxyphenylacetate, (6.5 g,0.018 mol) was added to a solution of the tin compound (11.2 mL, 0.022mol), lithium chloride (2.2 g, 0.051 mol), andtetrakis(triphenylphosphine)palladium(0) (410 mg, 0.35 mmol) in 90 mL ofanhydrous dioxane. The solution was heated to 85° C. for 191 hours. Theorganic layer was washed with brine, dried over magnesium sulfate, andfiltered. The solvent was removed by evaporation to afford a mixture ofproducts. Fraction two from a column chromatography (30% ethylacetate-hexane) afforded 3.8 g (48%) of an orange oil of the nitroproduct EX-21A; ¹H NMR ppm: 3.71 (m, 5H), 5.21 (s, 2H), 6.86 (bs, 1H),6.99 (m, 11H), 7.23 (d, 1H), 7.37 (m, 8H), 8.03 (t, 1H); ¹⁹F NMR ppm:−118.69 (m, 1F); HPLC purity (retention time): >99% (4.09 min); HRMScalcd for C₂₃H₁₉O₆N₂F₁ (M⁺+NH₄) 456.1571, found 456.1564. Fraction threeof the column chromatography (30% ethyl acetate-hexane) afforded 2.99 g(41%) of a brown solid of the aniline product EX-21B; ¹H NMR ppm: 3.64(d, 2H), 3.70 (s, 3H), 5.23 (s, 2H), 6.90 (m, 4H), 7.40 (m, 8H); ¹⁹F NMRppm: −136.68 (d, 1F); HPLC purity (retention time): >99% (3.50 min);HRMS calcd for C₂₃H₂₁O₄N₂F₁ (M⁺+NH₄) 426.1829, found 426.1846.

[0743] Sodium triacetoxyborohydride (5.6 g, 26.4 mmol) was added to asolution of the aniline EX-21B (2.69 g, 6.6 mmol), acetone (8.0 mL,excess), and a drop of acetic acid in a tetrahydrofuran-dichloromethane(1:1) solution. After stirring at room temperature for 26 hours, thesolution was diluted with ether and water. The organic layer was washedwith brine, dried over magnesium sulfate, and filtered. The solvent wasremoved by evaporation to afford the crude product. The product waspurified by column chromatography (30% ethyl acetate-hexane) to afford1.34 g (45%) of a white solid of the methyl ester N-isopropylanilineproduct EX-21C; ¹H NMR ppm: 1.30 (d, 6H), 3.62 (d, 2H), 3.68 (s, 3H),4.13 (m, 1H), 5.21 (s, 2H), 6.70 (m, 2H), 6.99 (m, 2H), 7.36 (m, 9H);HPLC purity (retention time): >99% (3.84 min); HRMS calcd forC₂₆H₂₇O₄N₂F₁ (M⁺+H) 451.2033, found 451.2023.

[0744] Aqueous sodium hydroxide (10%) (4.3 mL, 10.0 mmol) was added to asolution of the methyl ester EX-21C (1.21 g, 2.6 mmol) intetrahydrofuran and the resulting solution stirred at 60° C. for 48hours. Partial Cbz deprotection occurred so, benzyl chloroformate (382uL, 2.6 mmol) was added to the solution and the resulting solutionstirred at room temperature for 1 hour. The solution was acidified with2 N hydrochloric acid and extracted with diethyl ether. The solution waswashed with brine, dried over magnesium sulfate, and filtered. Thesolvent was removed by evaporation to afford the crude product. Theproduct was purified by column chromatography (50% ethyl acetate-hexane)to afford 0.24 g (21%) of a brown oil of the acetic acid product EX-21D;¹H NMR ppm: 1.28 (d, 6H), 3.65 (d, 2H), 4.12 (m, 1H), 5.19 (s, 2H), 6.69(m, 1H), 6.97 (m, 2H), 7.36 (m, 9H); HPLC purity (retention time): >99%(2.84 min).

[0745] PS-carbodiimide (1.00 mmol/g) (0.59 g, 0.59 mmol) was added to aslurry of the acid EX-21D (0.13 g, 0.29 mmole), 1-hydroxybenzotriazole(40.2 mg, 0.29 mmol), 4-(N-benzyloxycarbonylamidino) benzylaminehydrochloride (0.11 g, 0.34 mmol), and N-methylmorpholine (163 uL, 1.4mmol) in a dichloromethane-dimethylformamide (3:1) solution and thesuspension was agitated for 4 hours. Upon completion of the reaction,polyamine resin (2.81 mmol/g) (0.50 g, 1.4 mmol) and polymer-boundaldehyde (2.3 mmol/g) (0.050 g, 1.15 mmol) were added and the suspensionwas agitated for 1 hour. The solution was filtered, and the polymer wasrinsed with dimethylformamide and dichloromethane until no more UVactivity was seen in the dichloromethane washing. The combined filtrateand washings were evaporated to afford the crude product. The productEX-21E was carried on to the next step. HPLC purity (retention time):79% (2.77 min); HRMS calcd for C₄₁H₄₀O₅N₅F₁ (M⁺+H) 702.3092, found702.3114.

[0746] A catalytic amount of palladium on carbon (5%) in methanol wasadded to a methanol solution of the Cbz compound EX-21E (0.298 mmol),and the mixture was stirred under a balloon of hydrogen at roomtemperature until the reaction was complete. The mixture was filteredthrough celite, and the solvent was evaporated to afford the product.The product was purified by reverse-phase chromatography to afford 14.6mg (81%) of a white solid of the product; ¹H NMR ppm: 1.68 (d, 6H), 4.04(d, 2H), 4.15 (sept, 1H), 4.85 (d, 2H), 7.27 (m, 6H), 7.65 (t, 1H), 7.83(d, 2H), 8.07 (bt, 1H), 8.24 (d, 2H), 9.20 (bs, 1H), 10.38 (bs, 1H); ¹⁹FNMR ppm: −76.41 (s, 9F), −138.02 (d, 1F); HPLC purity (retentiontime): >99% (1.37 min); HRMS calcd for C₂₅H₂₉O₁N₅F₁ (M⁺+H) 434.2356,found 434.2360.

Example 22

[0747]

[0748] Sodium triacetoxyborohydride (93 g, 43.0 mmol) was added to asolution of the aniline, methyl2-[2-methoxy-3-amino-6-phenylphenyl]acetate, (2.99 g, 11.0 mmol),acetone (1.0 mL, 13.6 mmol), and a drop of acetic acid in atetrahydrofuran-dichloromethane (1:1) solution. After stirring at roomtemperature for 14 hours, additional acetone (1.0 mL, 13.6 mmol) andacetic acid (excess) was added, and the solution was stirred at roomtemperature for 18 hours. The solution was diluted with ether and water.The organic layer was washed with brine, dried over magnesium sulfate,and filtered. The solvent was removed by evaporation to afford the crudeproduct. The product was purified by column chromatography (15% ethylacetate-hexane) to afford 3.55 g (100%) of a yellow oil of the themethyl ester product EX-22A; ¹H NMR ppm: 1.24 (d, 6H), 3.59 (s, 3H),3.62 (m, 2H), 3.72 (s, 3H), 4.09 (m, 1H), 6.62 (d, 1H, J=8.3 Hz), 6.92(d, 1H, J=8.3 Hz), 7.28 (m, 5H); HPLC purity (retention time): 97.5%(2.57 min); HRMS calcd for C₁₉H₂₃O₃N₁ (M⁺+H) 314.1756, found 314.1758.

[0749] Aqueous sodium hydroxide (10%) (7.6 mL, 19.0 mmol) was added to asolution of the methyl ester EX-22A (1.51 g, 4.81 mmol) in methanol andthe resulting solution stirred at 60° C. for 3 hours. The solution wasacidified with 2 N hydrochloric acid and extracted with diethyl ether.The solution was washed with brine, dried over magnesium sulfate, andfiltered The solvent was removed by evaporation to afford the crudeproduct. The product was purified by column chromatography (40% ethylacetate-hexane) to afford 0.44 g (31%) of a white solid of thecarboxylic acid product EX-22B; ¹H NMR ppm: 1.25 (d, 6H), 3.62 (m, 3H),3.75 (s, 3H), 6.50 (d, 1H, J=8.3 Hz), 6.94 (d, 1H, J=8.3 Hz), 7.27 (m,5H); HPLC purity (retention time): >99% (2.11 min); HRMS calcd forC₁₈H₂₁O₃N₁ (M⁺+H) 300.1600, found 300.1587.

[0750] PS-carbodiimide (1.00 mmol/g) (2.8 g, 2.8 mmol) was added to aslurry of the acid EX-22B (0.42 g, 1.4 mmole), 1-hydroxybenzotriazole(0.19 mg, 1.4 mmol), 4-(N-benzyloxycarbonylamidino) benzylaminehydrochloride (0.54 g, 1.6 mmol), and N-methylmorpholine (620 uL, 5.6mmol) in a dichloromethane-dimethylformamide (3:1) solution, and thesuspension was agitated for 18 hours. Upon completion of the reaction,the polyamine resin (2.81 mmol/g) (1.0 g, 2.8 mmol) and polymer-boundaldehyde (2.3 mmol/g) (1.0 g, 2.30 mmol) were added, and the suspensionwas agitated for 1 hour. The solution was filtered, and the polymer wasrinsed with dimethylformamide and dichloromethane until no more UVactivity was seen in the dichloromethane washing. The combined filtrateand washings were evaporated to afford the crude product. The protectedproduct EX-22C was purified by column chromatography (60% ethylacetate-hexane) and then was washed off with 100% ethyl acetate toafford 0.73 g (92%) of a white solid EX-22C; ¹H NMR ppm: 1.25 (d, 6H),3.62 (m, 3H), 3.71 (s, 3H), 4.33 (d, 2H), 5.19 (s, 2H), 6.05 (bt, 1H),6.63 (d, 2H, J=8.3 Hz), 6.93 (d, 2H, J=8.3 Hz), 7.29 (m, 13H), 7.77 (d,2H); HPLC purity (retention time): >99% (2.55 min); HRMS calcd forC₃₄H₃₆O₄N₄ (M⁺+H) 565.2815, found 565.2839.

[0751] A catalytic amount of palladium on carbon (5%) in dioxane wasadded to 3 mL of a methanol-4N hydrochloric acid/dioxane (3:1) solutionof the Cbz compound EX-22C (50.0 mg, 0.88 mmol), and the mixture wasstirred under a balloon of hydrogen at room temperature for 12 hours.The mixture was filtered through celite, and the solvent was evaporatedto afford the product. The product was purified by reverse-phasechromatography to afford 22.0 mg (60%) of a purple-white solid; ¹H NMRppm: 1.41 (m, 6H), 3.65 (s, 2H), 3.82 (m, 1H), 3.95 (s, 3H), 4.39 (s,2H), 6.98 (d, 1H), 7.19 (d, 1H), 7.42 (m, 7H), 7.78 (d, 2H); HPLC purity(retention time): >99% (1.50 min); HRMS calcd for C₂₆H₃₀O₂N₄ (M⁺+H)431.2447, found 431.2447.

[0752] Using the disclosed examples and methods described herein, thefollowing further compounds having an amidinoaralkyl type Y⁰ group andvarious J-substituents can be prepared of the Formula:

[0753] wherein;

[0754] R² is 3-aminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0755] R² is 3-aminophenyl, B is phenyl, A is CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[0756] R² is 3-aminophenyl, B is 2-imidazoyl, A is CH₂CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0757] R² is 3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A isCH₂CH₂, is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0758] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro;

[0759] R² is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro;

[0760] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro;

[0761] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro;

[0762] R² is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0763] R² is 3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH₂CH₂,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0764] R² is 3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A isCH₂CH₂, is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[0765] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is hydrido;

[0766] R² is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is hydrido;

[0767] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is hydrido;

[0768] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is hydrido;

[0769] R² is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[0770] R² is 3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH₂CH₂,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[0771] R² is 3-aminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0772] R² is 3-aminophenyl, B is phenyl, A is CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0773] R² is 3-aminophenyl, B is 2-imidazoyl, A is CH₂CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0774] R² is 3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A isCH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0775] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro;

[0776] R² is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro;

[0777] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro;

[0778] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro;

[0779] R² is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0780] R² is 3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH₂CH₂,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0781] R² is 3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A isCH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0782] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is hydrido;

[0783] R² is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is hydrido;

[0784] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is hydrido;

[0785] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is hydrido;

[0786] R² is 3-diaminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0787] R² is 3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH₂CH₂,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0788] R² is 3-aminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0789] R² is 3-aminophenyl, B is (S)-2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0790] R² is amino-2-fluorophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0791] R² is 2-methyl-3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0792] R² is 3-aminophenyl, B is ethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0793] R² is 3-aminophenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0794] R² is 3-aminophenyl, B is 2-propenyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0795] R² is 3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0796] R² is 3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0797] R² is 3-aminophenyl, B is 2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0798] R² is 3-aminophenyl, B is (R)-2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0799] R² is 3-aminophenyl, B is 2-propynyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0800] R² is 3-aminophenyl, B is 3-pentyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0801] R¹ is 3-aminophenyl, B is hydrido, A is CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0802] R² is 3-aminophenyl, B is ethyl, A is CH₂, Y⁰ is 4-amidinobenzyl,J is hydroxy, and R¹ is chloro;

[0803] R² is 3-aminophenyl, B is 2-methypropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0804] R² is 3-aminophenyl, B is 2-propyl, A is CH₃CH, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0805] R² is 3-aminophenyl, B is propyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0806] R² is 3-aminophenyl, B is 6-amidocarbonylhexyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0807] R² is 3-aminophenyl, B is tert-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0808] R² is 3-aminophenyl, B is tert-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0809] R² is 3-aminophenyl, B is 3-hydroxypropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0810] R² is 3-aminophenyl, B is 2-methylpropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0811] R² is 3-aminophenyl, B is butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0812] R² is 3-aminophenyl, B is 1-methoxy-2-propyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0813] R² is 3-aminophenyl, B is 2-methoxyethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0814] R² is 3-aminophenyl, B is 2-propyl, A is a bond, Y⁰ is5-amidino-2-thienylmethyl, J is hydroxy, and R¹ is chloro;

[0815] R² is 5-amino-2-methylthiophenyl, B is 2-propyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0816] R² is 3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0817] R² is 3-amino-5-carbomethoxyphenyl, B is isopropyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0818] R² is 3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is bromo;

[0819] R² is 3-amino-5-carboxamidophenyl, B is isopropyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0820] R² is 3-amino-5-(N-benzyl-N-methylamidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0821] R² is 3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0822] R² is 3-amino-5-(N-(2-phenyl-2-propyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0823] R² is 3-amino-5-(N-(2,4-dichlorobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0824] R² is 3-amino-5-(N-(4-bromobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0825] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0826] R² is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0827] R² is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro;

[0828] R² is 3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0829] R² is 3-amino-5-(N-(3-trifluoromethylbenzyl)amidocarbonyl)phenyl,B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro;

[0830] R² is 3-amino-5-(N-isobutylamidocarbonyl)phenyl, B is isopropyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0831] R² is 3-amino-5-(N-cyclobutylamidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0832] R² is 3-amino-5-(N-cyclopentylamidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0833] R² is 3-amino-5-(N-cycloheptylamidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0834] R² is 3-amino-5-(N-(2-pyridylmethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0835] R² is 3-amino-5-(N-(3-pyridylmethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0836] R² is3-amino-5-(N-(2-(4-methoxyphenyl)ethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0837] R² is 3-amino-5-(N-(3-phenylpropyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0838] R² is 3-amino-5-(N-(2,2-diphenylethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0839] R² is 3-amino-5-(N-(2-naphthylmethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0840] R² is3-amino-5-(N-(1,2,3,4-tetrahydronaphth-2-ylmethyl)amidocarbonyl)phenyl,B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro;

[0841] R² is 3-aminophenyl, B is 2-propyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is hydrido;

[0842] R² is 3-carboxyphenyl, B is 2-propyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0843] R² is 3-aminophenyl, B is 2-propyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0844] R² is 3,5-diaminophenyl, B is 2,2,2-trifluoroethyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0845] R² is 3,5-diaminophenyl, B is (S)-2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0846] R² is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0847] R² is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzylbenzyl, J is hydroxy, and R¹ is chloro;

[0848] R² is 3,5-diaminophenyl, B is ethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0849] R² is 3,5-diaminopbenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0850] R² is 3-amino-5-carboxyphenyl, B is 2,2,2-trifluoroethyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0851] R² is 3-amino-5-carboxyphenyl, B is (S)-2-butyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0852] R² is 3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzylbenzyl, J is hydroxy, and R¹ is chloro;

[0853] R² is 3-amino-5-carboxyphenyl, B is ethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0854] R² is 3-amino-5-carboxyphenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0855] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is2,2,2-trifluoroethyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy,and R¹ is chloro;

[0856] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is (S)-2-butyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0857] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidino-2-fluorobenzylbenzyl, J is hydroxy, and R¹ ischloro;

[0858] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is abond, is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0859] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is abond, is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0860] R² is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzylbenzyl, J is hydroxy, and R¹ is hydrido;

[0861] R² is 3-aminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0862] R² is 3-aminophenyl, B is (S)-2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0863] R² is 5-amino-2-fluorophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0864] R² is 2-methyl-3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0865] R² is 3-aminophenyl, B is ethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0866] R² is 3-aminophenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0867] R² is 3-aminophenyl, B is 2-propenyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0868] R² is 3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0869] R² is 3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0870] R² is 3-aminophenyl, B is 2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0871] R² is 3-aminophenyl, B is (R)-2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0872] R² is 3-aminophenyl, B is 2-propynyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0873] R² is 3-aminophenyl, B is 3-pentyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[0874] R² is 3-aminophenyl, B is hydrido, A is CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0875] R² is 3-aminophenyl, B is ethyl, A is CH₂, Y⁰ is 4-amidinobenzyl,J is fluoro, and R¹ is chloro;

[0876] R² is 3-aminophenyl, B is 2-methypropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0877] R² is 3-aminophenyl, B is 2-propyl, A is CH₃CH, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0878] R² is 3-aminophenyl, B is propyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0879] R² is 3-aminophenyl, B is 6-amidocarbonylhexyl, A is a bond, Y⁰is 4-amidinobenzyl, J isfluoro, and R¹ is chloro;

[0880] R² is 3-aminophenyl, B is tert-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[0881] R² is 3-aminophenyl, B is tert-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0882] R² is 3-aminophenyl, B is 3-hydroxypropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0883] R² is 3-aminophenyl, B is 2-methylpropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0884] R² is 3-aminophenyl, B is butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0885] R² is 3-aminophenyl, B is 1-methoxy-2-propyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0886] R² is 3-aminophenyl, B is 2-methoxyethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0887] R² is 3-aminophenyl, B is 2-propyl, A is a bond, Y⁰ is5-amidino-2-thienylmethyl, J is fluoro, and R¹ is chloro;

[0888] R² is 5-amino-2-methylthiophenyl, B is 2-propyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0889] R² is 3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0890] R² is 3-amino-5-carbomethoxyphenyl, B is isopropyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0891] R² is 3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is bromo;

[0892] R² is 3-amino-5-carboxamidophenyl, B is isopropyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0893] R² is 3-amino-5-(N-benzyl-N-methylamidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0894] R² is 3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0895] R² is 3-amino-5-(N-(2-phenyl-2-propyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0896] R² is 3-amino-5-(N-(2,4-dichlorobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0897] R² is 3-amino-5-(N-(4-bromobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0898] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0899] R² is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0900] R² is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro;

[0901] R² is 3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0902] R² is 3-amino-5-(N-(3-trifluoromethylbenzyl)amidocarbonyl)phenyl,B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro;

[0903] R² is 3-amino-5-(N-isobutylamidocarbonyl)phenyl, B is isopropyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0904] R² is 3-amino-5-(N-cyclobutylamidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0905] R² is 3-amino-5-(N-cyclopentylamidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0906] R² is 3-amino-5-(N-cycloheptylamidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0907] R² is 3-amino-5-(N-(2-pyridylmethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0908] R² is 3-amino-5-(N-(3-pyridylmethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0909] R² is3-amino-5-(N-(2-(4-methoxyphenyl)ethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0910] R² is 3-amino-5-(N-(3-phenylpropyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0911] R² is 3-amino-5-(N-(2,2-diphenylethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0912] R² is 3-amino-5-(N-(2-naphthylmethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[0913] R² is3-amino-5-(N-(1,2,3,4-tetrahydronaphth-2-ylmethyl)amidocarbonyl)phenyl,B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro;

[0914] R² is 3-aminophenyl, B is 2-propyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is hydrido;

[0915] R² is 3-carboxyphenyl, B is 2-propyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[0916] R² is 3-aminophenyl, B is 2-propyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0917] R² is 3,5-diaminophenyl, B is 2,2,2-trifluoroethyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0918] R² is 3,5-diaminophenyl, B is (S)-2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0919] R² is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0920] R² is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzylbenzyl, J is fluoro, and R¹ is chloro;

[0921] R² is 3,5-diaminophenyl, B is ethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0922] R² is 3,5-diaminophenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0923] R² is 3-amino-5-carboxyphenyl, B is 2,2,2-trifluoroethyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0924] R² is 3-amino-5-carboxyphenyl, B is (S)-2-butyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0925] R² is 3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzylbenzyl, J is fluoro, and R¹ is chloro;

[0926] R² is 3-amino-5-carboxyphenyl, B is ethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0927] R² is 3-amino-5-carboxyphenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0928] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is2,2,2-trifluoroethyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro,and R¹ is chloro;

[0929] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is (S)-2-butyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0930] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidino-2-fluorobenzylbenzyl, J is fluoro, and R¹ ischloro;

[0931] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is abond, is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0932] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is abond, is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0933] R² is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzylbenzyl, J is fluoro, and R¹ is hydrido;

[0934] R² is 3-aminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0935] R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0936] R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0937] R² is 3-aminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0938] R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0939] R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0940] R² is 3-aminophenyl, B is cyclopentyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0941] R² is 5-amino-2-thienyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0942] R² is 3-aminophenyl, B is cyclopropyl, A is CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0943] R² is 3-aminophenyl, B is 2-(2R)-bicyclo[2.2.1]-heptyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0944] R² is 3-aminophenyl, B is cyclopentyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0945] R² is 3-aminophenyl, B is cyclohexyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0946] R² is 3-aminophenyl, B is oxalan-2-yl, A is CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0947] R² is 3-aminophenyl, B is 1-piperidinyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0948] R² is 3-aminophenyl, B is l-pyrrolidinyl, A is CH₂CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0949] R² is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0950] R² is 3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0951] R² is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0952] R² is 2-amino-6-carboxy-4-pyridyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0953] R² is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0954] R² is 3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0955] R² is 3,5-diaminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0956] R² is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0957] R² is 3,5-diaminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0958] R² is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0959] R² is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0960] R² is 3,5-diaminophenyl, B is cyclopentyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0961] R² is 3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0962] R² is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0963] R² is 3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y⁰is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0964] R² is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0965] R² is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro;

[0966] R² is 3-carboxy-5-aminophenyl, B is cyclopentyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0967] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0968] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, Ais a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ ischloro;

[0969] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0970] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl,A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ ischloro;

[0971] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido;

[0972] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, Ais a bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ ischloro;

[0973] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopentyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;

[0974] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0975] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy,and R¹ is chloro;

[0976] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0977] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy,and R¹ is chloro;

[0978] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ishydrido;

[0979] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is hydroxy,and R¹ is chloro;

[0980] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0981] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0982] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy,and R¹ is chloro;

[0983] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0984] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy,and R¹ is chloro;

[0985] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ishydrido;

[0986] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is hydroxy,and R¹ is chloro;

[0987] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro;

[0988] R² is 3-aminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0989] R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0990] R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidobenzyl, J is fluoro, and R¹ is chloro;

[0991] R² is 3-aminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0992] R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[0993] R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0994] R² is 3-aminophenyl, B is cyclopentyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0995] R² is 5-amino-2-thienyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0996] R² is 3-aminophenyl, B is cyclopropyl, A is CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0997] R² is 3-aminophenyl, B is 2-(2R)-bicyclo[2.2.1]-heptyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[0998] R² is 3-aminophenyl, B is cyclopentyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[0999] R² is 3-aminophenyl, B is cyclohexyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[1000] R² is 3-aminophenyl, B is oxalan-2-yl, A is CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1001] R² is 3-aminophenyl, B is 1-piperidinyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1002] R² is 3-aminophenyl, B is 1-pyrrolidinyl, A is CH₂CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1003] R² is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[1004] R² is 3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[1005] R² is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[1006] R² is 2-amino-6-carboxy-4-pyridyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[1007] R² is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1008] R² is 3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1009] R² is 3,5-diaminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1010] R² is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[1011] R² is 3,5-diaminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[1012] R² is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[1013] R² is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is chloro;

[1014] R² is 3,5-diaminophenyl, B is cyclopentyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1015] R² is 3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1016] R² is 3-carboxy-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[1017] R² is 3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y⁰is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;

[1018] R² is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[1019] R² is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is chloro;

[1020] R² is 3-carboxy-5-aminophenyl, B is cyclopentyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1021] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1022] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, Ais a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ ischloro;

[1023] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1024] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl,A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ ischloro;

[1025] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido;

[1026] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, Ais a bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is fluoro, and R¹ ischloro;

[1027] R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopentyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro;

[1028] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ iscbloro;

[1029] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro,and R¹ is chloro;

[1030] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[1031] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro,and R¹ is chloro;

[1032] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ishydrido;

[1033] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is fluoro,and R¹ is chloro;

[1034] R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[1035] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[1036] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro,and R¹ is chloro;

[1037] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro;

[1038] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro,and R¹ is chloro;

[1039] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ishydrido;

[1040] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is fluoro,and R¹ is chloro;

[1041] R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro.

[1042] Formula (I) compounds of this invention possessing hydroxyl,thiol, and amine functional groups can be converted to a wide varietyderivatives. A hydroxyl group in the form of an alcohol or phenol can bereadily converted to esters of carboxylic, sulfonic, carbarnic,phosphonic, and phosphoric acids. Acylation to form a carboxylic acidester is readily effected using a suitable acylating reagent such as analiphatic acid anhydride or acid chloride. The corresponding aryl andheteroaryl acid anhydrides and acid chlorides can also be used. Suchreactions are generally carried out using an amine catalyst such aspyridine in an inert solvent. Similarly, carbamic acid esters(urethanes) can be obtained by reacting a hydroxyl group withisocyanates and carbamoyl chlorides. Sulfonate, phosphonate, andphosphate esters can be prepared using the corresponding acid chlorideand similar reagents. Compounds of Formula (I) that have at least onethiol group present can be converted to the corresponding thioestersderivatives analogous to those of alcohols and phenols using the samereagents and comparable reaction conditions. Compounds of Formula (I)that have at least one primary or secondary amine group present can beconverted to the corresponding amide derivatives. Amides of carboxylicacids can be prepared using the appropriate acid chloride or anhydrideswith reaction conditions analogous to those used with alcohols andphenols. Ureas of the corresponding primary or secondary amine can beprepared using isocyanates directly and carbamoyl chlorides in thepresence of an acid scavenger such as triethylamine or pyridine.Sulfonamides can be prepared from the corresponding sulfonyl chloride inthe presence of aqueous sodium hydroxide. Suitable procedures andmethods for preparing these derivatives can be found in House's ModernSynthetic Reactions, W. A. Benjamin, Inc., Shriner, Fuson, and Curtin inThe Systematic Identification of Organic Compounds, 5th Edition, JohnWiley & Sons, and Fieser and Fieser in Reagents for Organic Synthesis,Volume 1, John Wiley & Sons. Reagents of a wide variety that can be usedto derivatize hydroxyl, thiol, and amines of compounds of Formula (I)are available from commercial sources or the references cited above,which are incorporated herein by reference.

[1043] Formula (I) compounds of this invention possessing hydroxyl,thiol, and amine functional groups can be alkylated to a wide varietyderivatives. A hydroxyl group of compounds of Formula (I) can be readilyconverted to ethers. Alkylation to form an ether is readily effectedusing a suitable alkylating reagent such as an alkyl bromide, alkyliodide or alkyl sulfonate. The corresponding aralkyl, heteroaralkyl,alkoxyalkyl, aralkyloxyalkyl, and heteroaralkyloxyalkyl bromides,iodides, and sulfonates can also be used. Such reactions are generallycarried out using an alkoxide forming reagent such as sodium hydride,potassium t-butoxide, sodium amide, lithium amide, and n-butyl lithiumusing an inert polar solvent such as DMF, DMSO, THF, and similar,comparable solvents amine catalyst such as pyridine in an inert solvent.Compounds of Formula (I) that have at least one thiol group present canbe converted to the corresponding thioether derivatives analogous tothose of alcohols and phenols using the same reagents and comparablereaction conditions. Compounds of Formula (I) that have at least oneprimary, secondary or tertiary amine group present can be converted tothe corresponding quaternary ammonium derivatives. Quaternary ammoniumderivatives can be prepared using the appropriate bromides, iodides, andsulfonates analogous to those used with alcohols and phenols. Conditionsinvolve reaction of the amine by warming it with the alkylating reagentwith a stoichiometric amount of the amine (i.e., one equivalent with atertiary amine, two with a secondary, and three with a primary). Withprimary and secondary amines, two and one equivalents, respectively, ofan acid scavenger are used concurrently. Tertiary amines can be preparedfrom the corresponding primary or secondary amine by reductivealkylation with aldehydes and ketones using reduction methods. Suitableprocedures and methods for preparing these derivatives can be found inHouse's Modem Synthetic Reactions, W. A. Benjamin, Inc., Shriner, Fuson,and Curtin in The Systematic Identification of Organic Compounds, 5thEdition, John Wiley & Sons, and Fieser and Fieser in Reagents forOrganic Synthesis, Volume 1, John Wiley & Sons. Perfluoroalkylderivatives can be prepared as described by DesMarteau in J. Chem. Soc.Chem. Commun. 2241 (1998). Reagents of a wide variety that can be usedto derivative hydroxyl, thiol, and amines of compounds of Formula (I)are available from commercial sources or the references cited above,which are incorporated herein by reference.

[1044] The biological activity of the compounds of Examples 1 through 22are summarized in the Table 2.

Assays for Biological Activity TF-VIIa Assay

[1045] In this assay 100 nM recombinant soluble tissue factor and 2 nMrecombinant human factor VIIa are added to a 96-well assay platecontaining 0.4 mM of the substrate,N-Methylsulfonyl-D-phe-gly-arg-p-nitroaniline and either inhibitor orbuffer (5 mM CaCl₂, 50 mM Tris-HCl, pH 8.0, 100 mM NaCl, 0.1% BSA). Thereaction, in a final volume of 100 ul is measured immediately at 405 nmto determine background absorbance. The plate is incubated at roomtemperature for 60 min, at which time the rate of hydrolysis of thesubstrate is measured by monitoring the reaction at 405 nm for therelease of p-nitroaniline. Percent inhibition of TF-VIIa activity iscalculated from OD_(405nm) value from the experimental and controlsample.

Xa Assay

[1046] 0.3 nM human factor Xa and 0.15 mMN-α-Benzyloxycarbonyl-D-arginyl-L-glycyl-L-arginine-p-nitroaniline-dihydrochloride(S-2765) are added to a 96-well assay plate containing either inhibitoror buffer (50 mM Tris-HCl, pH 8.0, 100 mM NaCl, 0.1% BSA). The reaction,in a final volume of 100 ul is measured immediately at 405 nm todetermine background absorbance. The plate is incubated at roomtemperaturefor 60 min, at which time the rate of hydrolysis of thesubstrate is measured by monitoring the reaction at 405 nm for therelease of p-nitroaniline. Percent inhibition of Xa activity iscalculated from OD_(405nm) value from the experimental and controlsample.

Thrombin Assay

[1047] 0.28 nM human thrombin and 0.06 mMH-D-Phenylalanyl-L-pipecolyl-L-arginine-p-nitroaniline dihydrochiorideare added to a 96-well assay plate containing either inhibitor or buffer(50 mM Tris-HCl, pH 8.0, 100 mM NaCl, 0.1% BSA). The reaction, in afinal volume of 100 ul is measured immediately at 405 nm to determinebackground absorbance. The plate is incubated at room temperature for 60min, at which time the rate of hydrolysis of the substrate is measuredby monitoring the reaction at 405 nm for the release of p-nitroaniline.Percent inhibition of thrombin activity is calculated from OD_(405nm)value from the experimental and control sample.

Trypsin Assay

[1048] 5 ug/ml trypsin, type IX from porcine pancreas and 0.375 mMN-α-Benzoyl-L-arginine-p-nitroanilide (L-BAPNA) are added to a 96-wellassay plate containing either inhibitor or buffer (50 mM Tris-HCl, pH8.0, 100 mM NaCl, 0.1% BSA). The reactions, in a final volume of 100 ulare measured immediately at 405 nm to determine background absorbance.The plate is incubated at room temperature for 60 min, at which time therate of hydrolysis of the substrate is measured by monitoring thereaction at 405 nm for the release of p-nitroaniline. Percent inhibitionof trypsin activity is calculated from OD_(405nm) value from theexperimental and control sample.

[1049] Recombinant soluble TF, consisting of amino acids 1-219 of themature protein sequence was expressed in E. coli and purified using aMono Q Sepharose FPLC. Recombinant human VIIa was purchased fromAmerican Diagnostica, Greenwich Conn. and chromogenic substrateN-Methylsulfonyl-D-phe-gly-arg-p-nitroaniline was prepared by AmericanPeptide Company, Inc., Sunnyvale, Calif. Factor Xa was obtained fromEnzyme Research Laboratories, South Bend Ind., thrombin from Calbiochem,La Jolla, Calif., and trypsin and L-BAPNA from Sigma, St. Louis Mo. Thechromogenic substrates S-2765 and S-2238 were purchased fromChromogenix, Sweden. TABLE 2 Inhibitory Activity of Substituted Benzenestoward Factor Xa, TF-VIIA, Thrombin II, and Trypsin II. Example TF-VIIAFactor Xa Thrombin II Trpysin II Number IC50 (uM) IC50 (uM) IC50 (uM)IC50 (uM) 1 >30 >30 >30 0.3 2 >30 >30 >30 >30 3 >30 >30 >30 >304 >30 >30 22% at 30 0.3 5 >30 7% at 30 43% at 30 236 >100 >100 >100 >100 7 >100 >100 >100 >100 8 >100 >100 >100 >1009 >30 >30 >30 0.3 10 >30 >30 >30 >30 11 >30 >30 >30 >3012 >30 >30 >30 >30 13 >30 >30 >30 >30 14 >30 >30 ≈30   7.315 >30 >30 >30 >30 16 16.4 1% at 30 1.6 0.8 17 4.0 >30 7.0 0.2 18 25 >309.5 0.5 19 2.7 >30 7.0 0.2 20 0.67 >30 9.0 0.2 21 0.34 18% 0.95 <0.04 2214.7 >30 7.9 0.10

What we claim is:
 1. A compound having the Formula (I):

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of hydrido, halo, hydroxy, hydroxyalkyl,amino, aminoalkyl, cyano, alkyl, alkenyl, haloalkyl, haloalkenyl,carboxy, carboxyalkyl, carboalkoxy, amidocarbonyl, acyl, phosphono,sulfo, O—R⁶, NH—R⁶, S—R⁶, S(O)—R⁶, and S(O)₂—R⁶, wherein R⁶ is selectedfrom the group consisting of alkyl, alkenyl, aryl, heteroaryl, aralkyl,heteroaralkyl, haloalkyl, haloalkenyl, acyl, aroyl, and heteroaroyl; Bis formula (V):

 wherein D¹, D², J¹, J² and K¹ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, no more than one of D¹, D², J¹, J² andK¹ is O, no more than one of D¹, D², J¹, J² and K¹ is S, one of D¹, D²,J¹, J² and K¹ must be a covalent bond when two of D¹, D², J¹, J² and K¹are O and S, and no more than four of D¹, D², J¹, J² and K¹ are N withthe proviso that R³², R³³, R³⁴, R³⁵, and R³⁶ are each independentlyselected to maintain the tetravalent nature of carbon, trivalent natureof nitrogen, the divalent nature of sulfur, and the divalent nature ofoxygen; R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected to beQ^(b); R⁹, R^(10, R) ¹¹, R¹², R¹³, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R³², R³³, R³⁴,R³⁵, and R³⁶ are independently selected from the group consisting ofhydrido, amidino, guanidino, dialkylsulfonium, trialkylphosphonium,dialkylsulfoniumalkyl, carboxy, heteroaralkylthio, heteroaralkoxy,cycloalkylamino, acylalkyl, acylalkoxy, aryloylalkoxy, heterocyclyloxy,aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl,perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl,aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl,cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl,cycloalkylsulfonylalkyl, heteroarylamino,N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio,alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy,cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy,cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy,halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl,hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio,alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl,heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl,arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl,heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl,haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido,alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkylamidosulfonyl, monoarylamidosulfonyl, arylsulfonamido,diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl, arylsulfinyl,arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl,heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl,heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl,alkynyl, alkenyloxy, alkenyloxyalky, alkylenedioxy, haloalkylenedioxy,cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower cycloalkylalkyl,lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, aminoalkyl,hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, aralkyl, atyloxy, aralkoxy,aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl,heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkyl,heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl,carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido,arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl,carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy,phosphono, phosphonoalkyl, diaralkoxyphosphono, anddiaralkoxyphosphonoalkyl; R³² and R³³, R³³ and R³⁴, R³⁴ and R³⁵, and R³⁵and R³⁶ substituent pairs are independently selected to form a spacerpair wherein a spacer pair is taken together to form a linear moietyhaving from 3 through 6 contiguous atoms connecting the points ofbonding of said spacer pair members to form a ring selected from thegroup consisting of a cycloalkenyl ring having 5 through 8 contiguousmembers, a partially saturated heterocyclyl ring having 5 through 8contiguous members, a heteroaryl ring having 5 through 6 contiguousmembers, and an aryl with the proviso that no more than one of the groupconsisting of spacer pairs R³² and R³³, R³³ and R³⁴, R³⁴ and R³⁵, andR³⁵ and R³⁶ are used at the same time; R⁹ and R¹⁰, R¹⁰ and R¹¹, R¹¹ andR¹², and R¹² and R¹³ spacer pairs are independently selected to form aspacer pair wherein a spacer pair is taken together to form a linearmoiety having from 3 through 6 contiguous atoms connecting the points ofbonding of said spacer pair members to form a ring selected from thegroup consisting of a cycloalkenyl ring having 5 through 8 contiguousmembers, a partially saturated heterocyclyl ring having 5 through 8contiguous members, a heteroaryl ring having 5 through 6 contiguousmembers, and an aryl with the proviso that no more than one of the groupconsisting of spacer pairs R⁹ and R¹⁰, R¹⁰ and R¹¹, R¹¹ and R¹², and R¹²and R¹³ is used at the same time; B is formula (VI):

 wherein D³, D⁴, J³, and J⁴ are independently selected from the groupconsisting of C, N, O, and S, no more than one of D³, D⁴, J³, and J⁴ isO, no more than one of D³, D⁴, J³, and J⁴ is S, and no more than threeof D¹, D², J¹, and J² are N with the proviso that R³², R³³, R³⁴, and R³⁵are each independently selected to maintain the tetravalent nature ofcarbon, trivalent nature of nitrogen, the divalent nature of sulfur, andthe divalent nature of oxygen; B is selected from the group consistingof C3-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8haloalkenyl wherein each member of group B may be optionally substitutedat any carbon up to and including 6 atoms from the point of attachmentof B to A with one or more of the group consisting of R₃₂, R₃₃, R₃₄,R₃₅, and R₃₆; B is selected from the group consisting of C3-C10cycloalkyl, C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9partially saturated heterocyclyl, wherein each ring carbon may beoptionally substituted with R₃₃, a ring carbon other than the ringcarbon at the point of attachment of B to A may be optionallysubstituted with oxo provided that no more than one ring carbon issubstituted by oxo at the same time, ring carbon and nitrogen atomsadjacent to the carbon atom at the point of attachment may be optionallysubstituted with R₉ or R₁₃, a ring carbon or nitrogen atom adjacent tothe R₉ position and two atoms from the point of attachment may besubstituted with R₁₀, a ring carbon or nitrogen atom adjacent to the R₁₃position and two atoms from the point of attachment may be substitutedwith R₁₂, a ring carbon or nitrogen atom three atoms from the point ofattachment and adjacent to the R₁₀ position may be substituted with R₁₁,a ring carbon or nitrogen atom three atoms from the point of attachmentand adjacent to the R₁₂ position may be substituted with R₃₃, and a ringcarbon or nitrogen atom four atoms from the point of attachment andadjacent to the R₁₁ and R₃₃ positions may be substituted with R₃₄; A isselected from the group consisting of single covalent bond,(W⁷)_(rr)—(CH(R¹⁵))_(pa) and (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is aninteger selected from 0 through 1, pa is an integer selected from 0through 6, and W⁷ is selected from the group consisting of O, S, C(O),C(S), C(O)S, C(S)O, C(O)N(R⁷), C(S)N(R⁷), (R⁷)NC(O), (R⁷)NC(S), S(O),S(O)₂, S(O)₂N(R⁷), (R⁷)NS(O)₂, Se(O), Se(O)₂, Se(O)₂N(R⁷), (R⁷)NSe(O)₂,P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), C(NR⁷)N(R⁷), (R⁷)NC(NR⁷), andN(R⁷) with the proviso that no more than one of the group consisting ofrr and pa are 0 at the same time; R⁷ and R⁸ are independently selectedfrom the group consisting of hydrido, hydroxy, alkyl, alkenyl, aryl,aralkyl, aryloxy, alkoxy, alkenyloxy, alkylthio, alkylamino, arylthio,arylamino, acyl, aroyl, heteroaroyl, aralkoxyalkyl, heteroaralkoxyalkyl,aryloxyalkyl, alkoxyalkyl, alkenyloxyalkyl, alkylthioalkyl,arylthioalkyl, aralkoxyalkyl, heteroaralkoxyalkyl, alkylsulfinylalkyl,alkylsulfonylalkyl, heteroaryl, heteroaryloxy, heteroarylamino,heteroaralkyl, heteroaralkyloxy, heteroaralkylamino, andheteroaryloxyalkyl; R¹⁴, R¹⁵, R³⁷, R³⁸, R³⁹, R⁴⁰, R⁴¹ and R⁴² areindependently selected from the group consisting of hydrido, hydroxy,halo, cyano, aryloxy, amino, alkylamino, dialkylamino, hydroxyalkyl,aminoalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, sulfhydryl,acylamido, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl,aralkyl, aryloxyalkyl, aralkoxyalkylalkoxy, alkylsulfinylalkyl,alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkoxythioalkyl,alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl,arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl,cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl,halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl,halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl,saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl,heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl,monocarboalkoxyalkyl, dicarboalkoxyalkyl, monocyanoalkyl, dicyanoalkyl,carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfinyl,haloalkylsulfonyl, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl,arylsulfonylalkyl, aralkylsulfinyl, aralkylsulfonyl, cycloalkylsulfinyl,cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl,heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl,heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl,carboxy, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl,carboaralkoxy, trialkylsilyl, dialkoxyphosphono, diaralkoxyphosphono,dialkoxyphosphonoalkyl, and diaralkoxyphosphonoalkyl with the provisothat R³⁷ and R³⁸ are independently selected from an acyl other thanformyl; R¹⁴ and R¹⁴, when bonded to different carbons, are takentogether to form a group selected from the group consisting of covalentbond, alkylene, haloalkylene, and a linear moiety spacer selected toform a ring selected from the group consisting of cycloalkyl ring havingfrom 5 through 8 contiguous members, cycloalkenyl ring having from 5through 8 contiguous members, and a heterocyclyl having from 5 through 8contiguous members; R¹⁴ and R¹⁵, when bonded to different carbons, aretaken together to form a group selected from the group consisting ofcovalent bond, alkylene, haloalkylene, and a linear moiety spacerselected to form a ring selected from the group consisting of acycloalkyl ring having from 5 through 8 contiguous members, acycloalkenyl ring having from 5 through 8 contiguous members, and aheterocyclyl having from 5 through 8 contiguous members; R¹⁵ and R¹⁵,when bonded to different carbons, are taken together to form a groupselected from the group consisting of covalent bond, alkylene,haloalkylene, and a linear moiety spacer selected to form a ringselected from the group consisting of cycloalkyl ring having from 5through 8 contiguous members, cycloalkenyl ring having from 5 through 8contiguous members, and a heterocyclyl having from 5 through 8contiguous members; Ψ is selected from the group consisting of NR⁵, O,C(O), C(S), S, S(O), S(O)₂, ON(R⁵), P(O)(R⁸), and CR³⁹R⁴⁰ with theprovisos that Ψ is selected from other than NR⁵, O, S, S(O), and S(O)₂unless any two of X⁰, R², R¹, and J are other than hydrido, or that Ψ isselected from other than O, unless A is selected from other thanmethylene when B is phenyl, that Ψ is selected from other than C(O),unless A is selected from other than methyleneoxy when B is phenyl, orthat Ψ is selected from other than NH unless A is selected from otherthan a single covalent bond when B is acyl, or that Ψ is selected fromother than NH unless A is selected from other than S(O) or S(O)₂ when Bis phenyl; R⁵ is selected from the group consisting of hydrido, alkyl,alkenyl, alkynyl, aryl, aralkyl, aryloxy, alkoxy, alkenyloxy, alkylthio,arylthio, aralkoxyalkyl, heteroaralkoxyalkyl, aryloxyalkyl, alkoxyalkyl,alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, aralkoxyalkyl,heteroaralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, cycloalkyl,cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl,haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl,haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxyalkyl,halocycloalkenyloxyalkyl, heteroaryl, heteroarylalkyl,monocarboalkoxyalkyl, monocarboalkoxy, dicarboalkoxyalkyl,monocarboxamido, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl,acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, anddialkoxyphosphonoalkyl; R³⁹ and R⁴⁰, when bonded to the same carbon, aretaken together to form a group selected from a group consisting of oxo,thiono, R⁵—N, alkylene, haloalkylene, and a linear moiety spacer havingfrom 2 through 7 contiguous atoms to form a ring selected from the groupconsisting of a cycloalkyl ring having from 3 through 8 contiguousmembers, a cycloalkenyl ring having from 3 through 8 contiguous members,and a heterocyclyl ring having from 3 through 8 contiguous members; X⁰,R² and R¹ are independently selected from the group consisting of Z⁰-Q,hydrido, alkyl, alkenyl, and halo; X⁰, R² and R¹ are independentlyselected from the group consisting of amidino, guanidino,dialkylsulfonium, trialkylphosphonium, dialkylsulfoniumalkyl,heteroarylamino, amino, nitro, alkylamino, arylamino, aralkylamino,alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl,haloalkanoyl, hydroxyhaloalkyl, cyano, and phosphono; X⁰ and R¹ aretaken together to form a spacer pair wherein the spacer pair forms alinear moiety having from 3 through 6 contiguous atoms connecting thepoints of bonding of said spacer pair members to form a ring selectedfrom the group consisting of a cycloalkenyl ring having from 5 through 8contiguous members and a partially saturated heterocyclyl ring havingfrom 5 through 8 contiguous members with the proviso that no more thanone of the group consisting of spacer pair X⁰ and R¹ and spacer pair R²and R¹ is used at the same time; X⁰ and R⁵ are taken together to form aspacer pair wherein the spacer pair forms a linear spacer moiety havingfrom 2 through 5 contiguous atoms connecting the points of bonding ofsaid spacer pair members to form a heterocyclyl ring having from 5through 8 contiguous members; X⁰ and R³⁹ are taken together to form aspacer pair wherein the spacer pair forms a linear spacer moiety havingfrom 2 through 5 contiguous atoms connecting the points of bonding ofsaid spacer pair members to form a heterocyclyl ring having from 5through 8 contiguous members; X⁰ and R⁴⁰ are taken together to form aspacer pair wherein the spacer pair forms a linear spacer moiety havingfrom 2 through 5 contiguous atoms connecting the points of bonding ofsaid spacer pair members to form a heterocyclyl ring having from 5through 8 contiguous members; X⁰ is selected to form a linear moietyhaving from 2 through 5 contiguous atoms linked to the points of bondingof both R³⁹ and R⁴⁰ to form a heterocyclyl ring having from 5 through 8contiguous members; R² and R¹ are taken together to form a spacer pairwherein the spacer pair forms a linear moiety having from 3 through 6contiguous atoms connecting the points of bonding of said spacer pairmembers to form a ring selected from the group consisting of acycloalkenyl ring having from 5 through 8 contiguous members and apartially saturated heterocyclyl ring having from 5 through 8 contiguousmembers with the proviso that no more than one of the group consistingof spacer pair X⁰ and R¹ and spacer pair R² and R¹ is used at the sametime; X⁰ and R¹ and R² and R¹ spacer pairs are selected independently tobe —W═X—Y═Z— forming a ring selected from the group consisting of aheteroaryl ring having from 5 through 6 contiguous members and an arylwith the proviso that no more than one of the group consisting of spacerpair X⁰ and R¹ and spacer pair R² and R¹ is used at the same time; W, X,Y, and Z are independently selected from the group consisting of C(R⁹),N, N(R¹⁰), O, S and a covalent bond with the provisos that W, X, Y, andZ are independently selected to be a covalent bond when one of W, X, Y,and Z is selected from the group consisting of O and S, no more than oneof W, X, Y, and Z is selected from the group consisting of O and S, nomore than three of W, X, Y, and Z are selected from the group consistingof N and N(R¹⁰), and C(R⁹), N, N(R¹⁰), O, and S are independentlyselected to maintain the tetravalent nature of carbon, trivalent natureof nitrogen, the divalent nature of sulfur, the divalent nature ofoxygen, and the aromaticity of the ring; R² and R^(4a), R² and R^(4b),R² and R¹⁴, and R² and R¹⁵ spacer pairs are independently selected toform spacer pairs wherein a spacer pair is taken together to form alinear moiety having from 2 through 5 contiguous atoms connecting thepoints of bonding of said spacer pair members to form a heterocyclylring having from 5 through 8 contiguous members with the proviso that nomore than one of the group of spacer pairs consisting of R² and R^(4a),R² and R^(4b), R² and R¹⁴, and R² and R¹⁵ is used at the same time; R²is independently selected to form a linear moiety having from 2 through5 contiguous atoms linked to the points of bonding of both R^(4a) andR^(4b) to form a heterocyclyl ring having from 5 through 8 contiguousmembers; Z⁰ is selected from the group consisting of covalent singlebond, (CR⁴¹R⁴²)_(q) wherein q is an integer selected from 1 through 6,(CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p) wherein g and p are integersindependently selected from 0 through 3 and W⁰ is selected from thegroup consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,C(O)N(R⁴¹), (R⁴¹)NC(O), C(S)N(R⁴¹), (R⁴¹)NC(S), OC(O)N(R⁴¹),(R⁴¹)NC(O)O, SC(S)N(R⁴¹), (R⁴¹)NC(S)S, SC(O)N(R⁴¹), (R⁴¹)NC(O)S,OC(S)N(R⁴¹), (R⁴¹)NC(S)O, N(R⁴²)C(O)N(R⁴¹), (R⁴¹)NC(O)N(R⁴²),N(R⁴²)C(S)N(R⁴¹), (R⁴¹)NC(S)N(R⁴¹), S(O), S(O)₂, S(O)₂N(R⁴¹),N(R⁴¹)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R⁴¹), N(R⁴¹)Se(O)₂, P(O)(R⁸),N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷)N(R⁴¹), ON(R⁴¹), and SiR²⁸R²⁹, and(CH(R⁴¹))_(e)—W²—(CH(R⁴²))_(h) wherein e and h are integersindependently selected from 0 through 2 and W² is selected from thegroup consisting of CR⁴¹═CR⁴², CR⁴¹R⁴²═C; vinylidene), and ethynylidene(C≡C; 1,2-ethynyl), with the provisos that R⁴¹ and R⁴² are selected fromother than halo and cyano when directly bonded to N and Z⁰ is directlybonded to the benzene ring, that W⁰ is selected, wherein g is 0, fromother than NHS(O)₂CH₂aryl or N(R⁴¹) unless R⁴¹ is selected from otherthan hydrido, alkyl, or aralkylsulfonyl, and Z⁰ is selected from otherthan OC(O), C(O)N(H), and (H)NC(O), unless Q is selected from other thanphenyl, 2-furyl, 2-thienyl, 4-thiazolyl, 2-pyridyl, 2-naphthyl,1,2-dihydrobenzofuran-5-yl, 1,2-dihydrobenzofuran-6-yl, or1,2-benzisoxazol-6-yl , or X⁰ is selected from other than hydrido, halo,or methyl, or R¹ is selected from other than hydrido, fluoro, hydroxy,acetoxy, propanoyloxy, 2-carboxyacetoxy, 2,3 or 4-carboxypropanoyloxy,benzoyloxy, methyl, or methoxy; R²⁸ and R²⁹ are independently selectedfrom the group consisting of hydrido, hydroxyalkyl, alkyl, alkenyl,alkynyl, aryl, aralkyl, aryloxyalkyl, acyl, aroyl, aralkanoyl,heteroaroyl, aralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl,aralkylthioalkyl, heteroaralkylthioalkyl, alkoxyalkyl,heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl,cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl,cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl,halocycloalkenyl, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy,halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryl,perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl,heteroarylthioalkyl, heteroaralkylthioalkyl, cyanoalkyl, dicyanoalkyl,carboxamidoalkyl, dicarboxamidoalkyl, cyanocarboalkoxyalkyl,carboalkoxyalkyl, dicarboalkoxyalkyl, cyanocycloalkyl,dicyanocycloalkyl, carboxamidocycloalkyl, dicarboxamidocycloalkyl,carboalkoxycyanocycloalkyl, carboalkoxycycloalkyl,dicarboalkoxycycloalkyl, formylalkyl, acylalkyl, arylsulfinylalkyl,arylsulfonylalkyl, aralkylsulfinyl, cycloalkylsulfinylalkyl,cycloalkylsufonylalkyl, heteroarylsulfonylalkyl,heteroarylsulfinylalkyl, aralkylsulfinylalkyl, aralkylsulfonylalkyl,carboxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyland diaralkoxyphosphonoalkyl; R²⁸ and R²⁹ are taken together to form alinear moiety spacer having from 2 through 7 contiguous atoms andforming a ring selected from the group consisting of a cycloalkyl ringhaving from 3 through 8 contiguous members, a cycloalkenyl ring havingfrom 3 through 8 contiguous members, and a heterocyclyl ring having from3 through 8 contiguous members; Q is formula (II):

 wherein D¹, D², J¹, J² and K¹ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, no more than one of D¹, D², J¹, J² andK¹ is O, no more than one of D¹, D², J¹, J² and K¹ is S, one of D¹, D²,J¹, J² and K¹ must be a covalent bond when two of D¹, D², J¹, J² and K¹are O and S, and no more than four of D¹, D², J¹, J² and K¹ are N, withthe proviso that R⁹ R¹⁰, R¹¹, R¹², and R¹³ are each independentlyselected to maintain the tetravalent nature of carbon, trivalent natureof nitrogen, the divalent nature of sulfur, and the divalent nature ofoxygen; Q is formula (III):

 wherein D³, D⁴, J³, and J⁴ are independently selected from the groupconsisting of C, N, O, and S, no more than one of D³, D⁴, J³, and J⁴ isO, no more than one of D³, D⁴, J³, and J⁴ is S, and no more than threeof D¹, D², J¹, and J² are N with the proviso that R⁹, R¹⁰, R¹¹, and R¹²are each independently selected to maintain the tetravalent nature ofcarbon, trivalent nature of nitrogen, the divalent nature of sulfur, andthe divalent nature of oxygen; Q is selected from the group consistingof alkyl, alkoxy, alkylamino, alkylthio, haloalkylthio, alkenyl,alkynyl, saturated heterocyclyl, partially saturated heterocyclyl, acyl,aroyl, heteroaroyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl,cycloalkenylalkyl, cycloalkylalkenyl, haloalkyl, haloalkoxy,haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl,haloalkenyloxyalkyl, halocycloalkoxyalkyl, and halocycloalkenyloxyalkylwith the proviso that Q is selected from other than than alkyl oralkenyl unless any one of X⁰, R¹, and J are other than hydrido; K is(CR^(4a)R^(4b))_(n) wherein n is an integer selected from 1 through 4;R^(4a) and R^(4b) are independently selected from the group consistingof halo, hydrido, hydroxy, cyano, hydroxyalkyl, alkyl, alkenyl, aryl,aralkyl, aralkoxyalkyl, aryloxyalkyl, alkoxyalkyl, heteroaryloxyalkyl,alkenyloxyalkyl, alkylthioalkyl, aralkylthioalkyl, arylthioalkyl,cycloalkyl, cycloalkylalkyl, haloalkyl, haloalkenyl, heteroaryl,heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl,cyanoalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, haloalkylsulfinyl,arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfonylalkyl,heteroarylsulfinylalkyl, aralkylsulfinylalkyl, and aralkylsulfonylalkyl;R^(4a) and R^(4b), when bonded to the same carbon, are taken together toform a group selected from the group consisting of oxo, thiono, and alinear spacer moiety having from 2 through 7 contiguous atoms connectedto form a ring selected from the group consisting of a cycloalkyl ringhaving 3 through 8 contiguous members, a cycloalkenyl ring having 5through 8 contiguous members, and a heterocyclyl ring having 5 through 8contiguous members; E⁰ is E¹, when K is (CR^(4a)R^(4b))_(n), wherein E¹is selected from the group consisting of a covalent single bond, O, S,C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷),(R⁷)NC(S), OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷),(R⁷)NC(O)S, OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸),N(R⁸)C(S)N(R⁷), (R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂,S(O)₂N(R⁷)C(O), C(O)N(R⁷)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R⁷),N(R⁷)Se(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁸), N(R⁷), ON(R⁷),SiR²⁸R²⁹, CR^(4a)═CR^(4b), ethynylidene (C≡C; 1,2-ethynyl), andC═CR^(4a)R^(4b); K is (CH(R¹⁴))_(j)-T wherein j is selected from ainteger from 0 through 3 and T is selected from the group consisting ofsingle covalent bond, O, S, and N(R⁷) with the proviso that(CH(R¹⁴))_(j) is bonded to the phenyl ring; E⁰ is E², when K is(CH(R¹⁴))_(j)-T, wherein E² is selected from the group consisting of acovalent single bond, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R⁷),(R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S), (R⁷)NC(O)O, (R⁷)NC(S)S, (R⁷)NC(O)S,(R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷),(R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, S(O)₂N(H)C(O),C(O)N(H)S(O)₂, Se(O), Se(O)₂, Se(O)₂N(R⁷), N(R⁷)Se(O)₂, P(O)(R⁸),N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), and N(R⁷); K is G-(CH(R¹⁵))_(k) wherein kis selected from an integer from 1 through 3 and G is selected from thegroup consisting of O, S, and N(R⁷) with the proviso that R¹⁵ is otherthan hydroxy, cyano, halo, amino, alkylamino, dialkylamino, andsulfhydryl when k is 1; E⁰ is E³ when K is G-(CH(R¹⁵))_(k) wherein E³ isselected from the group consisting of a covalent single bond, O, S,C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷),(R⁷)NC(S), OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷),(R⁷)NC(O)S, OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸),N(R⁸)C(S)N(R⁷), (R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, Se,Se(O), Se(O)₂, Se(O)₂N(R⁷), N(R⁷)Se(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸),P(O)(R⁸)N(R⁷), N(R⁷), ON(R⁷), SiR²⁸R²⁹, CR^(4a)═CR^(4b), ethynylidene(C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b); Y⁰ is formula (IV):

 wherein D⁵, D⁶, J⁵, and J⁶ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, K² is independently selected from thegroup consisting of C, and N⁺, no more than one of D⁵, D⁶, J⁵, and J⁶ isO, no more than one of D⁵, D⁶, J⁵, and J⁶ is S, one of D⁵, D⁶, J⁵, andJ⁶ must be a covalent bond when two of D⁵, D⁶, J⁵, and J⁶ are O and S,no more than three of D⁵, D⁶, J⁵, and J⁶ are N when K² is N⁺, and nomore than four of D⁵, D⁶, J⁵, and J⁶ are N when K² is carbon with theprovisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are each independently selected tomaintain the tetravalent nature of carbon, trivalent nature of nitrogen,the divalent nature of sulfur, and the divalent nature of oxygen; R¹⁶and R¹⁷ are independently taken together to form a linear moiety. spacerhaving from 3 through 6 contiguous atoms connected to form a ringselected from the group consisting of a cycloalkenyl ring having from 5through 8 contiguous members, a partially saturated heterocyclyl ringhaving from 5 through 8 contiguous members, a heteroaryl having from 5through 6 contiguous members, and an aryl; R¹⁸ and R¹⁹ are independentlytaken together to form a linear moiety spacer having from 3 through 6contiguous atoms connected to form a ring selected from the groupconsisting of a cycloalkenyl ring having from 5 through 8 contiguousmembers, a partially saturated heterocyclyl ring having from 5 through 8contiguous members, a heteroaryl having from 5 through 6 contiguousmembers, and an aryl; Q^(b) is selected from the group consisting ofNR²⁰R²¹, ⁺NR²⁰R²¹R²², oxy, alkyl, alkylaminoalkyl, aminoalkyl,dialkylsulfoniumalkyl, and acylamino wherein R²⁰, R²¹, and R²² areindependently selected from the group consisting of hydrido, alkyl,hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkylwith the provisos that no more than one of R²⁰, R²¹, and R²² is hydroxy,alkoxy, alkylamino, amino, and dialkylamino and that R²⁰, R²¹, and R²²must be other than be hydroxy, alkoxy, alkylamino, amino, anddialkylamino when K² is N⁺; R²⁰ and R²¹, R²⁰ and R²², and R²¹ and R²²pairs are independently selected to form a spacer pair wherein a spacerpair is taken together to form a linear moiety having from 4-through 7contiguous atoms connecting the points of bonding of said spacer pairmembers to form a heterocyclyl ring having 5 through 8 contiguousmembers with the proviso that no more than one of the group consistingof spacer pairs R²⁰ and R²¹, R²⁰ and R²², and R²¹ and R²² is used at thesame time; Q^(b) is selected from the group consisting ofN(R²⁶)SO₂N(R²³)(R²⁴), N(R²⁶)C(O)OR⁵, N(R²⁶)C(O)SR⁵, N(R²⁶)C(S)OR⁵ andN(R²⁶)C(S)SR⁵ with the proviso that no more than one of R²³, R²⁴, andR²⁶ are hydroxy, alkoxy, alkylamino, amino, or dialkylamino when two ofthe group consisting of R²³, R²⁴, and R²⁶ are bonded to the same atom;Q^(b) is selected from the group consisting of dialkylsulfonium,trialkylphosphonium, C(NR²⁵)NR²³R²⁴, N(R²⁶)C(NR²⁵R²³)(R²⁴),N(R²⁶)C(O)N(R²³)(R²⁴), N(R²⁶)C(S)N(R²³)(R²⁴)C(NR²⁵)OR⁵,C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(S)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO²N(R²³)(R²⁴), C(NR²⁵)SR⁵,C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with the provisos that no more than one ofR²³, R²⁴, and R²⁶ is hydroxy, alkoxy, alkyl amino, amino, ordialkylamino when two of the group consisting of R²³, R²⁴, and R²⁶ arebonded to the same atom and that said Q^(b) group is bonded directly toa carbon atom; R²³, R²⁴, R²⁵, and R²⁶ are independently selected fromthe group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino,dialkylamino, aminoalkyl, and hydroxyalkyl; R²³ and R²⁴ are takentogether to form a linear spacer moiety having from 4 through 7contiguous atoms connecting the points of bonding to form a heterocyclylring having 5 through 8 contiguous members; R²³ and R²⁵, R²⁴ and R²⁵,R²⁵ and R²⁶, R²⁴ and R²⁶, and R²³ and R²⁶ pairs are independentlyselected to form a spacer pair wherein a spacer pair is taken togetherfrom the points of bonding of selected spacer pair members to form thegroup L—U—V wherein L, U, and V are independently selected from thegroup consisting of O, S, C(O), C(S), C(J_(H))₂ S(O), SO₂, OP(OR³¹)R³⁰,P(O)R³⁰, P(S)R³⁰, C(R³⁰)R³¹, C═C(R³⁰)R³¹, (O)₂POP(O)₂, R³⁰(O)POP(O)R³⁰,Si(R²⁹)R²⁸, Si(R²⁹)R²⁸Si(R²⁹)R²⁸, Si(R²⁹)R²⁸OSi(R²⁹)R²⁸,(R²⁸)R²⁹COC(R²⁸)R²⁹, (R²⁸)R²⁹CSC(R²⁸)R²⁹, C(O)C(R³⁰)═C(R³¹),C(S)C(R³⁰)═C(R³¹), S(O)C(R³⁰)═C(R³¹), SO²C(R³⁰)═C(R³¹),PR³⁰C(R³⁰)═C(R³¹), P(O)R³⁰C(R³⁰)═C(R³¹), P(S)R³⁰C(R³⁰)═C(R³¹),DC(R³⁰)(R³¹)D, OP(OR³¹)R³⁰, P(O)R³⁰, P(S)R³⁰, Si(R²⁸)R²⁹ and N(R³⁰), anda covalent bond with the proviso that no more than any two of L, U and Vare simultaneously covalent bonds and the heterocyclyl comprised of byL, U, and V has from 5 through 10 contiguous member; D is selected fromthe group consisting of oxygen, C═O, C═S, S(O)_(m) wherein m is aninteger selected from 0 through 2; J_(H) is independently selected fromthe group consisting of OR²⁷, SR²⁷ and N(R²⁰)R²¹; R²⁷ is selected fromthe group consisting of hydrido, alkyl, alkenyl, alkynyl, aralkyl,aryloxyalkyl, aralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl,aralkylthioalkyl, heteroaralkylthioalkyl, alkoxyalkyl,heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl,cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl,cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl,halocycloalkenyl, haloalkoxyalkyl, haloalkenyloxyalkyl,halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, perhaloaryloxyalkyl,heteroaryl, heteroarylalkyl, heteroarylthioalkyl,heteroaralkylthioalkyl, arylsulfinylalkyl, arylsulfonylalkyl,cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl,heteroarylsulfonylalkyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyland aralkylsulfonylalkyl; R³⁰ and R³¹ are independently selected fromhydrido, hydroxy, thiol, aryloxy, amino, alkylamino, dialkylamino,hydroxyalkyl, heteroaryloxyalkyl, alkoxy, alkylthio, arylthio, alkyl,alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, aralkoxyalkyl,alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl,heteroaralkoxythioalkyl, alkoxyalkyl, heteroaryloxyalkyl,alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl,cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl,haloalkyl, haloalkenyl, haloaralkylsulfinylalkyl, aralkylsulfonylalkyl,cyanoalkyl, dicyanoalkyl, carboxamidoalkyl, dicarboxamidoalkyl,cyanocarboalkoxyalkyl, carboalkoxyalkyl, dicarboalkoxyalkyl,cyanocycloalkyl, dicyanocycloalkyl, carboxamidocycloalkyl,dicarboxamidocycloalkyl, carboalkoxycyanocycloalkyl,carboalkoxycycloalkyl, dicarboalkoxycycloalkyl, formylalkyl, acylalkyl,dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, phosphonoalkyl,dialkoxyphosphonoalkoxy, diaralkoxyphosphonoalkoxy, phosphonoalkoxy,dialkoxyphosphonoalkylamino, diaralkoxyphosphonoalkylamino,phosphonoalkylamino, dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl,sulfonylalkyl, alkoxysulfonylalkyl, aralkoxysulfonylalkyl,alkoxysulfonylalkoxy, aralkoxysulfonylalkoxy, sulfonylalkoxy,alkoxysulfonylalkylamino, aralkoxysulfonylalkylamino, andsulfonylalkylamino; R³⁰ and R³¹ are taken to form a linear moiety spacergroup having from 2 through 7 contiguous atoms to form a ring selectedfrom the group consisting of a cycloalkyl ring having from 3 through 8contiguous members, a cycloalkenyl ring having from 3 through 8contiguous members, and a heterocyclyl ring having from 3 through 8contiguous members; R²³ and R²⁵, R²⁴ and R²⁵, R²⁵ and R²⁶, R²⁴ and R²⁶,and R²³ and R²⁶ pairs are independently selected to form a spacer pairwherein a spacer pair is taken together from the points of bonding ofselected spacer pair members to form the group L—U—V wherein L, U, and Vare independently selected from the group of 1,2-disubstituted radicalsconsisting of a cycloalkyl radical, a cycloalkenyl radical whereincycloalkyl and cycloalkenyl radicals are substituted with one or moregroups selected from R³⁰ and R³¹, an aryl radical, an heteroarylradical, a saturated heterocyclic radical and a partially saturatedheterocyclic radical wherein said 1,2-substitutents are independentlyselected from C═O, C═S, C(R²⁸)R³², S(O), S(O)₂, OP(OR³¹)R³⁰, P(O)R³⁰,P(S)R³⁰ and Si(R²⁸)R²⁹; R²³ and R²⁵, R²⁴ and R²⁵, R²⁵ and R²⁶, R²⁴ andR²⁶, and R²³ and R²⁶ pairs are independently selected to form a spacerpair wherein a spacer pair is taken together from the points of bondingof selected spacer pair members to form the group L-U-V wherein L, U,and V are independently selected from the group of radicals consistingof 1,2-disubstituted alkylene radicals and 1,2-disubstituted alkenyleneradical wherein said 1,2-substitutents are independently selected fromC═O, C═S, C(R²⁸)R²⁹, S(O), S(O)₂, OP(OR³¹)R³⁰, P(O)R³⁰, P(S)R³⁰, andSi(R²⁸)R²⁹ and said alkylene and alkenylene radical are substituted withone or more R³⁰ or R³¹ substituents; Q^(s) is selected from the groupconsisting of a single covalent bond, (CR³⁷R³⁸)_(b)—(W⁰)_(az) wherein azis an integer selected from 0 through 1, b is an integer selected from 1through 4, and W⁰ is selected from the group consisting of O, S, C(O),C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴),(R¹⁴)NC(S), OC(O)N(R¹⁴), SC(S)N(R¹⁴), SC(O)N(R¹⁴), OC(S)N(R¹⁴),N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵),S(O), S(O)₂, S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R¹⁷),N(R¹⁴)Se(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴),and SiR²⁸R²⁹, (CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d areintegers independently selected from 1 through 4, and W¹ is selectedfrom the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S,C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴),(R¹⁴)NC(O)O, SC(S)N(R¹⁴), (R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S,OC(S)N(R¹⁴), (R¹⁴)NC(S)O, N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵),N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵), S(O), S(O)₂, S(O)₂N(R¹⁴),N(R¹⁴)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R¹⁴), N(R¹⁴)Se(O)₂, P(O)(R⁸),N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴) SiR²⁸R²⁹, and(CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) wherein e and h are integersindependently selected from 0 through 2 and W² is selected from thegroup consisting of CR^(4a)═CR^(4b), ethynylidene (C≡C; 1,2-ethynyl),and C═CR^(4a)R^(4b) with the provisos that R¹⁴ and R¹⁵ are selected fromother than halo and cyano when directly bonded to N and that(CR³⁷R³⁸)_(b), (CH(R¹⁴))_(c), (CH(R¹⁴))_(e) and are bonded to E⁰; R³⁷and R³⁷, when bonded to different carbons, are taken together to form alinear moiety spacer having from 1 through 7 contiguous atoms to form aring selected from the group consisting of a cycloalkyl ring having from3 through 8 contiguous members, a cycloalkenyl ring having from 3through 8 contiguous members, and a heterocyclyl ring having from 3through 8 contiguous members; R³⁷ and R³⁸, when bonded to differentcarbons, are taken together to form a linear moiety spacer having from 1through 7 contiguous atoms to form a ring selected from the groupconsisting of a cycloalkyl ring having from 3 through 8 contiguousmembers, a cycloalkenyl ring having from 3 through 8 contiguous members,and a heterocyclyl ring having from 3 through 8 contiguous members; R³⁸and R³⁸, when bonded to different carbons, are taken together to form alinear moiety spacer having from 1 through 7 contiguous atoms to form aring selected from the group consisting of a cycloalkyl ring having from3 through 8 contiguous members, a cycloalkenyl ring having from 3through 8 contiguous members, and a heterocyclyl ring having from 3through 8 contiguous members; R³⁷ and R³⁸, when bonded to the samecarbon, are taken together to form a group selected from a groupconsisting of oxo, thiono, alkylene, haloalkylene, and a linear moietyspacer having from 2 through 7 contiguous atoms to form a ring selectedfrom the group consisting of a cycloalkyl ring having from 3 through 8contiguous members, a cycloalkenyl ring having from 3 through 8contiguous members, and a heterocyclyl ring having from 3 through 8contiguous members; Y⁰ is Q^(b)-Q^(ss) wherein Q^(ss) is selected fromthe group consisting of (CR³⁷R³⁸)_(f) wherein f is an integer selectedfrom 1 through 6, (CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d areintegers independently selected from 1 through 4, and W¹ is selectedfrom the group consisting of W¹ is selected from the group consisting ofO, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O),C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴), (R¹⁴)NC(O)O, SC(S)N(R¹⁴),(R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S, OC(S)N(R¹⁴), (R¹⁴)NC(S)O,N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵) N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵),S(O), S(O)₂, S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, Se, Se(O), Se(O)₂, Se(O)₂N(R¹⁴),N(R¹⁴)Se(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴),SiR²⁸R²⁹, and (CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) wherein e and h areintegers independently selected from 0 through 2 and W² is selected fromthe group consisting of CR^(4a)═CR^(4b), ethynylidene (C≡C;1,2-ethynyl), and C═CR^(4a)R^(4b) with the provisos that R¹⁴ and R¹⁵ areselected from other than halo and cyano when directly bonded to N andthat (CR³⁷R³⁸)_(f), (CH(R¹⁵))_(c), and (CH(R¹⁵))_(e) are bonded to E⁰;Y⁰ is Q^(b)-Q^(sss) wherein Q^(sss) is (CH(R³⁸))_(r)—W³, r is an integerselected from 1 through 3, and W³ is selected from the group consistingof 1,1-cyclopropyl, 1,2-cyclopropyl, 1,1-cyclobutyl, 1,2-cyclobutyl,1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl,1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl,2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl,1,3-piperazinyl, 1,4-piperazinyl, 2,3-piperazinyl, 2,5-piperazinyl,2,6-piperazinyl, 1,2-pipcidinyl, 1,3-piperidinyl, 1,4-piperidinyl,2,3-piperidinyl, 2,4-piperidinyl, 2,5-piperidinyl, 2,6-piperidinyl,3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl, 1,2-pyrrolidinyl,1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl,3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl, 2H-2,5-pyranyl,4H-2,3-pyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl,2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl,2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl,2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl,2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and 3,5-tetrahydropyranylwith the proviso that (CH(R³⁸))_(r) is bonded to E⁰ and Q^(b) is bondedto lowest numbered substituent position of each W³; Y⁰ is Q^(b)-Q^(sssr)wherein Q^(sssr) is (CH(R³⁸))_(r)—W⁴, r is an integer selected from 1through 3, and W⁴ is selected from the group consisting of1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl,1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl,2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl,1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl, 2,3-piperazinyl,2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl,1,4-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,5-piperidinyl,2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl,1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl,2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl,2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl,2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl,2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl,3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl,2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and3,5-tetrahydropyranyl with the provisos that (CH(R³⁸))_(r) is bonded toE⁰ and Q^(b) is bonded to highest number substituent position of eachW⁴; Y⁰ is Q^(b)-Q^(ssss) wherein Q^(ssss) is (CH(R³⁸))_(r)—W⁵, r is aninteger selected from 1 through 3, and W⁵ is selected from the groupconsisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl,3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl,3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to lowest number substituent position of each W⁵ andthat (CH(R³⁸))_(r) is bonded to E⁰; Y⁰ is Q^(b)-Q^(ssssr) whereinQ^(ssssr) is (CH(R³⁸))_(r)—W⁶, r is an integer selected from 1 through3, and W⁶ is selected from the group consisting of 1,4-indenyl,1-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl,2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl,3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl,2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl,3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl,2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl,3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl,2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl,3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl,1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl,2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl,3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl,2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl,3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl,1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl,2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl,2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl,2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl,3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl,4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl,1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl,3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl,3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl,4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl,3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl,4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl withthe proviso that Q^(b) is bonded to highest number substituent positionof each W⁶ and that (CH(R³⁸))_(r) is bonded to E⁰.
 2. The compound asrecited in claim 1 or a pharmaceutically acceptable salt thereof,wherein; J is selected from the group consisting of hydrido, halo,hydroxy, hydroxyalkyl, amino, aminoalkyl, cyano, alkyl, haloalkyl,carboxy, carboxyalkyl, carboalkoxy, amidocarbonyl, acyl, phosphono,sulfo, O—R⁶, NH—R⁶, S—R⁶, S(O)—R⁶, and S(O)₂—R⁶, wherein R⁶ is selectedfrom the group consisting of alkyl, and haloalkyl, haloalkenyl; B isformula (V):

 wherein D¹, D², J¹, J² and K¹ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, no more than one of D¹, D², J¹, J² andK¹ is O, no more than one of D¹, D², J¹, J² and K¹ is S, one of D¹, D²,J¹, J² and K¹ must be a covalent bond when two of D¹, D², J¹, J² and K¹are O and S, and no more than four of D¹, D², J¹, J² and K¹ are N withthe proviso that R³², R³³, R³⁴, R³⁵, and R³⁶ are each independentlyselected to maintain the tetravalent nature of carbon, trivalent natureof nitrogen, the divalent nature of sulfur, and the divalent nature ofoxygen; R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected to beQ^(b); R⁹, R¹⁰, R¹¹, R¹², R¹³, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R³², R³³, R³⁴, R³⁵,and R³⁶ are independently selected from the group consisting of hydrido,amidino, guanidino, dialkylsulfonium, trialkylphosphonium,dialkylsulfoniumalkyl, carboxy, heteroaralkylthio, heteroaralkoxy,cycloalkylamino, acylalkyl, acylalkoxy, aryloylalkoxy, heterocyclyloxy,aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl,perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl,aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl,cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl,cycloalkylsulfonylalkyl, heteroarylamino,N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio,alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy,cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl, cycloalkylalkoxy,cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy,halocycloalkoxyalkyl, halocycloalkenyloxy, halocycloalkenyloxyalkyl,hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio,alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl,heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl,arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl,heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl,haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido,alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkylamidosulfonyl, monoarylamidosulfonyl, arylsulfonamido,diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl, arylsulfinyl,arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl,heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl,heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl,alkynyl, alkenyloxy, alkenyloxyalky, alkylenedioxy, haloalkylenedioxy,cycloalkyl, cycloalkylalkanoyl, cycloalkenyl, lower cycloalkylalkyl,lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, aminoalkyl,hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, aralkyl, aryloxy, aralkoxy,aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl,heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkyl,heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl,carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido,arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl,carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy,phosphono, phosphonoalkyl, diaralkoxyphosphono, anddiaralkoxyphosphonoalkyl; R³² and R³³, R³³ and R³⁴, R³⁴ and R³⁵, and R³⁵and R³⁶ pairs are independently selected to form a spacer pair wherein aspacer pair is taken together to form a linear moiety having from 3through 6 contiguous atoms connecting the points of bonding of saidspacer pair members to form a ring selected from the group consisting ofa cycloalkenyl ring having 5 through 8 contiguous members, a partiallysaturated heterocyclyl ring having 5 through 8 contiguous members, aheteroaryl ring having 5 through 6 contiguous members, and an aryl withthe proviso that no more than one of the group consisting of spacerpairs R³² and R³³, R³³ and R³⁴, R³⁴ and R³⁵, and R³⁵ and R³⁶ is used atthe same time; R⁹ and R¹⁰, R¹⁰ and R¹¹, R¹¹ and R¹², and R¹² and R¹³pairs are independently selected to form a spacer pair wherein a spacerpair is taken together to form a linear moiety having from 3 through 6contiguous atoms connecting the points of bonding of said spacer pairmembers to form a ring selected from the group consisting of acycloalkenyl ring having 5 through 8 contiguous members, a partiallysaturated heterocyclyl ring having 5 through 8 contiguous members, aheteroaryl ring having 5 through 6 contiguous members, and an aryl withthe proviso that no more than one of the group consisting of spacerpairs R⁹ and R¹⁰, R¹⁰ and R¹¹, R¹¹ and R¹², and R¹² and R¹³ is used atthe same time; B is selected from the group consisting of C3-C8 alkyl,C3-C8 alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8 haloalkenylwherein each member of group B may be optionally substituted at anycarbon up to and including 6 atoms from the point of attachment of B toA with one or more of the group consisting of R₃₂, R₃₃, R₃₄, R₃₅, andR₃₆; B is selected from the group consisting of C3-C10 cycloalkyl,C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9 partiallysaturated heterocyclyl, wherein each ring carbon may be optionallysubstituted with R₃₃, a ring carbon other than the ring carbon at thepoint of attachment of B to A may be optionally substituted with oxoprovided that no more than one ring carbon is substituted by oxo at thesame time, ring carbon and nitrogen atoms adjacent to the carbon atom atthe point of attachment may be optionally substituted with R₉ or R₁₃, aring carbon or nitrogen atom adjacent to the R₉ position and two atomsfrom the point of attachment may be substituted with R₁₀, a ring carbonor nitrogen atom adjacent to the R₁₃ position and two atoms from thepoint of attachment may be substituted with R₁₂, a ring carbon ornitrogen atom three atoms from the point of attachment and adjacent tothe R₁₀ position may be substituted with R₁₁, a ring carbon or nitrogenatom three atoms from the point of attachment and adjacent to the R₁₂position may be substituted with R₃₃, and a ring carbon or nitrogen atomfour atoms from the point of attachment and adjacent to the R₁₁ and R₃₃positions may be substituted with R₃₄; A is selected from the groupconsisting of single covalent bond, (W⁷)_(rr)—(CH(R¹⁵))_(pa) and(CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is an integer selected from 0through 1, pa is an integer selected from 0 through 6, and W⁷ isselected from the group consisting of O, S, C(O), C(S), C(O)S, C(S)O,C(O)N(R⁷), C(S)N(R⁷), (R⁷)NC(O), (R⁷)NC(S), S(O), S(O)₂, S(O)₂N(R⁷),(R⁷)NS(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), C(NR⁷)N(R⁷),(R⁷)NC(NR⁷), and N(R⁷) with the proviso that no more than one of thegroup consisting of rr and pa is 0 at the same time; R⁷ and R⁸ areindependently selected from the group consisting of hydrido, hydroxy,alkyl, acyl, aroyl, heteroaroyl, and alkoxyalkyl; R¹⁴, R¹⁵, R³⁷, and R³⁸are independently selected from the group consisting of hydrido,hydroxy, halo, cyano, hydroxyalkyl, alkoxy, alkyl, alkoxyalkyl,cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl,haloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl,halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl,carboxy, carboxyalkyl, carboalkoxy, carboxamide, and carboxamidoalkyl; Ψis selected from the group consisting of NR⁵, O, C(O), C(S), S, S(O),S(O)₂, ON(R⁵), P(O)(R⁸), and CR³⁹R⁴⁰ with the provisos that Ψ isselected from other than NR⁵, O, S, S(O), and S(O)₂ unless any two ofX⁰, R², R¹, and J are other than hydrido, or that Ψ is selected fromother than O, unless A is selected from other than methylene when B isphenyl, that Ψ is selected from other than C(O), unless A is selectedfrom other than methyleneoxy when B is phenyl, or that Ψ is selectedfrom other than NH unless A is selected from other than a singlecovalent bond when B is acyl, or that Ψ is selected from other than NHunless A is selected from other than S(O) or S(O)₂ when B is phenyl; R⁵is selected from the group consisting of hydrido, alkyl, alkoxy,alkoxyalkyl, haloalkyl, acyl, aroyl, and heteroaroyl; R³⁹ and R⁴⁰ areindependently selected from the group consisting of hydrido, hydroxy,halo, cyano, hydroxyalkyl, acyl, aroyl, heteroaroyl, acylamido, alkoxy,alkyl, alkoxyalkyl, haloalkyl, haloalkoxy, haloalkoxyalkyl,alkylsulfonyl, haloalkylsulfonyl, carboxy, carboxyalkyl, carboalkoxy,carboxamide, and carboxamidoalkyl; X⁰, R² and R¹ are independentlyselected from the group consisting of Z⁰-Q, hydrido, alkyl, alkenyl, andhalo; X⁰, R² and R¹ are independently selected from the group consistingof amidino, guanidino, dialkylsulfonium, trialkylphosphonium,dialkylsulfoniumalkyl, heteroarylamino, amino, nitro, alkylamino,arylamino, aralkylamino, alkanoyl, alkenoyl, aroyl, heteroaroyl,aralkanoyl, heteroaralkanoyl, haloalkanoyl, hydroxyhaloalkyl, cyano, andphosphono; X⁰ and R¹ are taken together to form a spacer pair whereinthe spacer pair forms a linear moiety having from 3 through 6 contiguousatoms connecting the points of bonding of said spacer pair members toform a ring selected from the group consisting of a cycloalkenyl ringhaving from 5 through 8 contiguous members and a partially saturatedheterocyclyl ring having from 5 through 8 contiguous members with theproviso that no more than one of the group consisting of spacer pair X⁰and R¹ and spacer pair R² and R¹ is used at the same time; R² and R¹ aretaken together to form a spacer pair wherein the spacer pair forms alinear moiety having from 3 through 6 contiguous atoms connecting thepoints of bonding of said spacer pair members to form a ring selectedfrom the group consisting of a cycloalkenyl ring having from 5 through 8contiguous members and a partially saturated heterocyclyl ring havingfrom 5 through 8 contiguous members with the proviso that no more thanone of the group consisting of spacer pair X⁰ and R¹ and spacer pair R²and R¹ is used at the same time; X⁰ and R¹ and R² and R¹ spacer pairsare selected independently to be —W═X—Y═Z— forming a ring selected fromthe group consisting of a heteroaryl ring having from 5 through 6contiguous members and an aryl with the proviso that no more than one ofthe group consisting of spacer pair X⁰ and R¹ and spacer pair R² and R¹is used at the same time; W, X, Y, and Z are independently selected fromthe group consisting of C(R⁹), N, N(R¹⁰), O, S and a covalent bond withthe provisos that one of W, X, Y, and Z is independently selected to bea covalent bond when one of W, X, Y, and Z is selected from the groupconsisting of O and S, no more than one of W, X, Y, and Z is selectedfrom the group consisting of O and S, no more than three of W, X, Y, andZ are selected from the group consisting of N and N(R¹⁰), and C(R⁹), N,N(R¹⁰), O, and S are independently selected to maintain the tetravalentnature of carbon, trivalent nature of nitrogen, the divalent nature ofsulfur, the divalent nature of oxygen, and the aromaticity of the ring;Z⁰ is selected from the group consisting of covalent single bond,(CR⁴¹R⁴²)_(q) wherein q is an integer selected from 1 through 6,(CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p) wherein g and p are integersindependently selected from O through 3 and W⁰ is selected from thegroup consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,C(O)N(R⁴¹), (R⁴¹)NC(O), C(S)N(R⁴¹), (R⁴¹)NC(S), OC(O)N(R⁴¹),(R⁴¹)NC(O)O, SC(S)N(R⁴¹), (R⁴¹)NC(S)S, SC(O)N(R⁴¹), (R⁴¹)NC(O)S,OC(S)N(R⁴¹), (R⁴¹)NC(S)O, N(R⁴²)C(O)N(R⁴¹), (R⁴¹)NC(O)N(R⁴²),N(R⁴²)C(S)N(R⁴¹), (R⁴¹)NC(S)N(R⁴²), S(O), S(O)₂, S(O)₂N(R⁴¹),N(R⁴¹)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R⁴¹), ON(R⁴¹),and (CH(R⁴¹))_(e)—W²—(CH(R⁴²))_(h) wherein e and h are integersindependently selected from O through 2 and W² is selected from thegroup consisting of CR⁴¹═CR⁴², CR⁴¹R⁴²═C; vinylidene), and ethynylidene(C≡C; 1,2-ethynyl), with the provisos that R⁴¹ and R⁴² are selected fromother than halo and cyano when directly bonded to N and Z⁰ is directlybonded to the benzene ring, that W⁰ is selected, wherein g is 0, fromother than NHS(O)₂CH₂aryl or N(R⁴¹) unless R⁴¹ is selected from otherthan hydrido, alkyl, or aralkylsulfonyl, and Z⁰ is selected from otherthan OC(O), C(O)N(H), and (H)NC(O), unless Q is selected from other thanphenyl, 2-furyl, 2-thienyl, 4-thiazolyl, 2-pyridyl, 2-naphthyl,1,2-dihydrobenzofuran-5-yl, 1,2-dihydrobenzofuran-6-yl, or1,2benzisoxazol-6-yl , or X⁰ is selected from other than hydrido, halo,or methyl, or R¹ is selected from other than hydrido, fluoro, hydroxy,acetoxy, propanoyloxy, 2-carboxyacetoxy, 2,3 or 4-carboxypropanoyloxy,benzoyloxy, methyl, or methoxy; R⁴¹ and R⁴² are independently selectedfrom the group consisting of hydrido, hydroxy, halo, cyano, aryloxy,hydroxyalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, alkoxy,alkyl, aryl, aralkyl, aryloxyalkyl, aralkoxyalkylalkoxy, alkoxyalkyl,heteroaryloxyalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl,cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl,halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl,halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl,saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl,heteroaralkyl, heteroarylthioalkyl, heteroaralkylthioalkyl,alkylsulfonyl, haloalkylsulfonyl, arylsulfonyl, arylsulfonylalkyl,aralkylsulfonyl, cycloalkylsulfonyl, cycloalkylsufonylalkyl,heteroarylsulfonylalkyl, heteroarylsulfonyl, and aralkylsulfonylalkyl; Qis formula (II):

 wherein D¹, D², J¹, J² and K¹ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, no more than one of D¹, D², J¹, J² andK¹ is O, no more than one of D¹, D², J¹, J² and K¹ is S, one of D¹, D²,J¹, J² and K¹ must be a covalent bond when two of D¹, D², J¹, J² and K¹are O and S, and no more than four of D¹, D², J¹, J² and K¹ are N, withthe proviso that R⁹, R¹⁰, R¹¹, R¹², and R¹³ are each independentlyselected to maintain the tetravalent nature of carbon, trivalent natureof nitrogen, the divalent nature of sulfur, and the divalent nature ofoxygen; Q is formula (III):

 wherein D³, D⁴, J³, and J⁴ are independently selected from the groupconsisting of C, N, O, and S, no more than one of D³, D⁴, J³, and J⁴ isO, no more than one of D³, D⁴, J³, and J⁴ is S, and no more than threeof D¹, D², J¹, and J² are N with the proviso that R⁹, R¹⁰, R¹¹, and R¹²are each independently selected to maintain the tetravalent nature ofcarbon, trivalent nature of nitrogen, the divalent nature of sulfur, andthe divalent nature of oxygen; Q is selected from the group consistingof alkyl, alkoxy, alkylamino, alkylthio, haloalkylthio, alkenyl,alkynyl, saturated heterocyclyl, partially saturated heterocyclyl, acyl,aroyl, heteroaroyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl,cycloalkenylalkyl, cycloalkylalkenyl, haloalkyl, haloalkoxy,haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl,haloalkenyloxyalkyl, halocycloalkoxyalkyl, and halocycloalkenyloxyalkylwith the proviso that Q is selected from other than than alkyl oralkenyl unless any one of X⁰, R¹ and J is other than hydrido; K is(CR^(4a)R^(4b))_(n) wherein n is an integer selected from 1 through 2;R^(4a) and R^(4b) are independently selected from the group consistingof halo, hydrido, hydroxy, cyano, hydroxyalkyl, alkyl, alkenyl,alkoxyalkyl, haloalkyl, haloalkenyl, and cyanoalkyl; R^(4a) and R^(4b),when bonded to the same carbon, are taken together to form a groupselected from the group consisting of oxo, and a linear spacer moietyhaving from 2 through 7 contiguous atoms connected to form a ringselected from the group consisting of a cycloalkyl ring having 3 through8 contiguous members, a cycloalkenyl ring having 5 through 8 contiguousmembers, and a heterocyclyl ring having 5 through 8 contiguous members;E⁰ is E¹, when K is (CR^(4a)R^(4b))_(n), wherein E¹ is selected from thegroup consisting of a covalent single bond, O, S, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷), (R⁷)NC(O)S,OC(S)N(R), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷),(R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, S(O)₂N(R⁷)C(O),C(O)N(R⁷)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R⁷), ON(R⁷),CR^(4a)═CR^(4b), ethynylidene (C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b); Kis (CH(R¹⁴))_(j)-T wherein j is selected from a integer from 0 through 2and T is selected from the group consisting of single covalent bond, O,S, and N(R⁷) with the proviso that (CH(R¹⁴))_(j) is bonded to the phenylring; E⁰ is E², when K is (CH(R¹⁴))_(j)-T, wherein E² is selected fromthe group consisting of a covalent single bond, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),(R⁷)NC(O)O, (R⁷)NC(S)S, (R⁷)NC(O)S, (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷),(R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷), (R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷),N(R⁷)S(O)₂, S(O)₂N(H)C(O), C(O)N(H)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸),P(O)(R⁸)N(R⁷), and N(R⁷); K is G-(CH(R¹⁵))_(k) wherein k is selectedfrom an integer from 1 through 2 and G is selected from the groupconsisting of O, S, and N(R⁷) with the proviso that R¹⁵ is other thanhydroxy, cyano, halo, amino, alkylamino, dialkylamino, and sulfhydrylwhen k is 1; E⁰ is E³, when K is G-(CH(R¹⁵))_(k), wherein E³ is selectedfrom the group consisting of a covalent single bond, O, S, C(O), C(S),C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷), (R⁷)NC(O)S,OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷),(R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, P(O)(R⁸),N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷), N(R⁷), ON(R⁷), CR^(4a)═CR^(4b),ethynylidene (C≡C; 1,2-ethynyl), and C═C^(4a)R^(4b); Y⁰ is formula (IV):

 wherein D⁵, D⁶, J⁵, and J⁶ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, K² is independently selected from thegroup consisting of C, and N⁺, no more than one of D⁵, D⁶, J⁵, and J⁶ isO, no more than one of D⁵, D⁶, J⁵, and J⁶ is S, one of D⁵, D⁶, J⁵, andJ⁶ must be a covalent bond when two of D⁵, D⁶, J⁵, and J⁶ are O and S,no more than three of D⁵, D⁶, J⁵, and J⁶ are N when K² is N⁺, and nomore than four of D⁵, D⁶, J⁵, and J⁶ are N when K² is carbon with theprovisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are each independently selected tomaintain the tetravalent nature of carbon, trivalent nature of nitrogen,the divalent nature of sulfur, and the divalent nature of oxygen; R¹⁶and R¹⁷ are taken together to form a linear moiety spacer having from 3through 6 contiguous atoms connected to form a ring selected from thegroup consisting of a cycloalkenyl ring having from 5 through 8contiguous members, a partially saturated heterocyclyl ring having from5 through 8 contiguous members, a heteroaryl having from 5 through 6contiguous members, and an aryl; Q^(b) is selected from the groupconsisting of NR²⁰R²¹, ⁺NR²⁰R²¹R²², oxy, alkyl, alkylaminoalkyl,aminoalkyl, dialkylsulfoniumalkyl, and acylamino wherein R²⁰, R²¹, andR²² are independently selected from the group consisting of hydrido,alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, andhydroxyalkyl with the provisos that no more than one of R²⁰, R²¹, andR²² is hydroxy, alkoxy, alkylamino, amino, and dialkylamino and thatR²⁰, R²¹, and R²² must be other than be hydroxy, alkoxy, alkylamino,amino, and dialkylamino when K² is N⁺; R²⁰ and R²¹, R²⁰ and R²², and R²¹and R²² pairs are independently selected to form a spacer pair wherein aspacer pair is taken together to form a linear moiety having from 4through 7 contiguous atoms connecting the points of bonding of saidspacer pair members to form a heterocyclyl ring having 5 through 8contiguous members with the proviso that no more than one of the groupconsisting of spacer pairs R²⁰ and R²¹, R²⁰ and R²², and R²¹ and R²² isused at the same time; Q^(b) is selected from the group consisting ofN(R²⁶)SO²N(R²³)(R²⁴), N(R²⁶)C(O)OR⁵, N(R²⁶)C(O)SR⁵, N(R²⁶)C(S)OR⁵ andN(R²⁶)C(S)SR⁵ with the proviso that no more than one of R²³, R²⁴, andR²⁶ is hydroxy, alkoxy, alkylamino, amino, or dialkylamino when two ofthe group consisting of R²³, R²⁴, and R²⁶ are bonded to the same atom;Q^(b) is selected from the group consisting of dialkylsulfonium,trialkylphosphonium, C(NR²⁵)NR²³R²⁴, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)C(O)N(R²³)(R²⁴), N(R²⁶)C(S)N(R²³)(R²⁴), C(NR²⁵)OR⁵,C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(S)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO²N(R²³)(R²⁴), C(NR²⁵)SR⁵,C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with the provisos that no more than one ofR²³, R²⁴, and R²⁶ is hydroxy, alkoxy, alkylamino, amino, or dialkylaminowhen two of the group consisting of R²³, R²⁴, and R²⁶ are bonded to thesame atom and that said Q^(b) group is bonded directly to a carbon atom;R²³, R²⁴, R²⁵, and R²⁶ are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino,aminoalkyl, and hydroxyalkyl; R²³ and R²⁴ are taken together to form alinear spacer moiety having from 4 through 7 contiguous atoms connectingthe points of bonding to form a heterocyclyl ring having 5 through 8contiguous members; Q^(s) is selected from the group consisting of asingle covalent bond, (CR³⁷R³⁸)_(b)—(W⁰)_(az) wherein az is an integerselected from 0 through 1, b is an integer selected from 1 through 4,and W⁰ is selected from the group consisting of O, S, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴), (R¹⁴)NC(S),OC(O)N(R¹⁴), SC(S)N(R¹⁴), SC(O)N(R¹⁴) OC(S)N(R¹⁴), N(R¹⁵)C(O)N(R¹⁴),(R¹⁴)NC(O)N(R¹⁵) N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵), S(O), S(O)₂,S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸), P(O)(R⁸)N(R⁷),N(R¹⁴), ON(R¹⁴), (CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d areintegers independently selected from 1 through 4, and W¹ is selectedfrom the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S,C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴),(R¹⁴)NC(O)O, SC(S)N(R¹⁴), (R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S,OC(S)N(R¹⁴), (R¹⁴)NC(S)O, N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵),N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵), S(O), S(O)₂, S(O)₂N(R¹⁴),N(R¹⁴)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸) P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴), and(CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) wherein e and h are integersindependently selected from 0 through 2 and W² is selected from thegroup consisting of CR^(4a)═CR^(4b), ethynylidene (C≡C; 1,2-ethynyl),and C═CR^(4a)R^(4b) with the provisos that R¹⁴ and R¹⁵ are selected fromother than halo and cyano when directly bonded to N and that(CR³⁷R³⁸)_(b), (CH(R¹⁴))_(c), (CH(R¹⁴))_(e) and are bonded to E⁰; Y⁰ isQ^(b)-Q^(ss) wherein Q^(ss) is selected from the group consisting of(CR³⁷R³⁸)_(f) wherein f is an integer selected from 1 through 6,(CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 4, and W¹ is selected from thegroup consisting of W¹ is selected from the group consisting of O, S,C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O),C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴), (R¹⁴)NC(O)O, SC(S)N(R¹⁴),(R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S, OC(S)N(R¹⁴), (R¹⁴)NC(S)O,N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵),S(O), S(O)₂, S(O)₂N(R¹⁴) N(R¹⁴)S(O)₂, P(O)(R⁸), N(R⁷)P(O)(R⁸),P(O)(R⁸)N(R⁷), N(R¹⁴), ON(R¹⁴), and (CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h)wherein e and h are integers independently selected from 0 through 2 andW² is selected from the group consisting of CR^(4a)═CR^(4b),ethynylidene (C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b) with the provisosthat R¹⁴ and R¹⁵ are selected from other than halo and cyano whendirectly bonded to N and that (CR³⁷R³⁸)_(f), (CH(R¹⁵))_(c), and(CH(R¹⁵))_(e) are bonded to E⁰; Y⁰ is Q^(b)-Q^(sss), wherein Q^(sss) is(CH(R³⁸))_(r)—W³, r is an integer selected from 1 through 3, and W³ isselected from the group consisting of 1,1-cyclopropyl, 1,2-cyclopropyl,1,1-cyclobutyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl,1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl,2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl,3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl,2,3-piperazinyl, 2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl,1,3-piperidinyl, 1,4-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl,2,5-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl,3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl,2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl,2H-2,4-pyranyl, 2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl,4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl,4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl,2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl,2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl,3,4-tetrahydropyranyl, and 3,5-tetrahydropyranyl with the proviso that(CH(R³⁸))_(r) is bonded to E⁰ and Q^(b) is bonded to lowest numberedsubstituent position of each W³; Y⁰ is Q^(b)-Q^(sssr), wherein Q^(sssr)is (CH(R³⁸))_(r)—W⁴, r is an integer selected from 1 through 3, and W⁴is selected from the group consisting of 1,2-cyclobutyl, 1,2-cyclohexyl,1,3-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl,2,3-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl,3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl,1,4-piperazinyl, 2,3-piperazinyl, 2,5-piperazinyl, 2,6-piperazinyl,1,2-piperidinyl, 1,3-piperidinyl, 1,4-piperidinyl, 2,3-piperidinyl,2,4-piperidinyl, 2,5-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl,3,5-piperidinyl, 3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl,2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl,2H-2,3-pyranyl, 2H-2,4-pyranyl, 2H-2,5-pyranyl, 4H-2,3-pyranyl,4H-2,4-pyranyl, 4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl,2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl,2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl,2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl,2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and 3,5-tetrahydropyranylwith the provisos that (CH(R³⁸))_(r) is bonded to E⁰ and Q^(b) is bondedto highest number substituent position of each W⁴; Y⁰ is Q^(b)-Q^(ssss),wherein Q^(ssss) is (CH(R³⁸))_(r)—W⁵, r is an integer selected from 1through 3, and W⁵ is selected from the group consisting of 1,4-indenyl,1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl,2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl,3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl,2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl,3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl,2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl,3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl,2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl,3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl,1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl,2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl,3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl,2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl,3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl,1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl,2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl,2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl,2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl,3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl,4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl,1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl,3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl,3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl,4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl,3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl,4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl withthe proviso that Q^(b) is bonded to lowest number substituent positionof each W⁵ and that (CH(R³⁸))_(r) is bonded to E⁰; Y⁰ isQ^(b)-Q^(ssssr), wherein Q^(ssssr) is (CH(R³⁸))_(r)—W⁶ an integerselected from 1 through 3, and W⁶ is selected from the group consistingof 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl,2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl,3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl,2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl,3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl,2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl,3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl,3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl,3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl,1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl,2,6-isoindolyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl,3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl,2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl,3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl,3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl,1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl,2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyl,2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl, 3,4-quinolinyl,3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl,4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl,1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to highest number substituent position of each W⁶ andthat (CH(R³⁸))_(r) is bonded to E⁰.
 3. The compound as recited in claim1 or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of hydrido, halo, hydroxy, hydroxyalkyl,amino, aminoalkyl, cyano, haloalkyl, carboxy, carboxyalkyl,amidocarbonyl, acyl, O—R⁶, NH—R⁶, S—R⁶, wherein R⁶ is selected from thegroup consisting of alkyl and haloalkyl; B is formula (V):

 wherein D¹, D², J¹, J² and K¹ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, no more than one of D¹, D², J¹, J² andK¹ is O, no more than one of D¹, D², J¹, J² and K¹ is S, one of D¹, D²,J¹, J² and K¹ must be a covalent bond when two of D¹, D², J¹, J² and K¹are O and S, and no more than four of D¹, D², J¹, J² and K¹ are N; R³²,R³³, R³⁴, R³⁵, and R³⁶ are independently selected to be Q^(b); R⁹, R¹⁰,R¹¹, R¹², R¹³, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R³², R³³, R³⁴, R³⁵, and R³⁶ areindependently selected from the group consisting of hydrido, amidino,guanidino, dialkylsulfonium, trialkylphosphonium, dialkylsulfoniumalkyl,carboxy, heteroaralkylthio, heteroaralkoxy, cycloalkylamino, acylalkyl,acylalkoxy, aryloylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl,aralkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl,aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl,halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl,cycloalkylsulfinylalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl,heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl,haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl,heteroaralkoxy, cycloalkoxy, cycloalkenyloxy, cycloalkoxyalkyl,cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy,halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxy,halocycloalkenyloxyalkyl, hydroxy, amino, alkoxyamino, thio, nitro,lower alkylamino, alkylthio, alkylthioalkyl, arylamino, aralkylamino,arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl,alkylsulfinylalkyl, arylsulfinylalkyl, arylsulfonylalkyl,heteroarylsulfinylalkyl, heteroarylsulfonylalkyl, alkylsulfonyl,alkylsulfonylalkyl, haloalkylsulfinylalkyl, haloalkylsulfonylalkyl,alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkylamidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl,arylsulfonamido, diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl,arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl,heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl,alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl,haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky,alkylenedioxy, haloalkylenedioxy, cycloalkyl, cycloalkylalkanoyl,cycloalkenyl, lower cycloalkylalkyl, lower cycloalkenylalkyl, halo,haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl,hydroxyalkyl, aminoalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl,aralkyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl,partially saturated heterocyclyl, heteroaryl, heteroaryloxy,heteroaryloxyalkyl, arylalkyl, heteroarylalkyl, arylalkenyl,heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido,alkylamidocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl,carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano,carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, anddiaralkoxyphosphonoalkyl; B is selected from the group consisting ofC3-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8haloalkenyl wherein each member of group B may be optionally substitutedat any carbon up to and including 6 atoms from the point of attachmentof B to A with one or more of the group consisting of R₃₂, R₃₃, R₃₄,R₃₅, and R₃₆; B is selected from the group consisting of C3-C10cycloalkyl, C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9partially saturated heterocyclyl, wherein each ring carbon may beoptionally substituted with R₃₃, a ring carbon other than the ringcarbon at the point of attachment of B to A may be optionallysubstituted with oxo provided that no more than one ring carbon issubstituted by oxo at the same time, ring carbon and nitrogen atomsadjacent to the carbon atom at the point of attachment may be optionallysubstituted with R₉ or R₁₃, a ring carbon or nitrogen atom adjacent tothe R₉ position and two atoms from the point of attachment may besubstituted with R₁₀, a ring carbon or nitrogen atom adjacent to the R₁₃position and two atoms from the point of attachment may be substitutedwith R₁₂, a ring carbon or nitrogen atom three atoms from the point ofattachment and adjacent to the R₁₀ position may be substituted with R¹¹,a ring carbon or nitrogen atom three atoms from the point of attachmentand adjacent to the R₁₂ position may be substituted with R₃₃, and a ringcarbon or nitrogen atom four atoms from the point of attachment andadjacent to the R₁₁ and R₃₃ positions may be substituted with R₃₄; A isselected from the group consisting of single covalent bond,(W⁷)_(rr)—(CH(R¹⁵))_(pa) and (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is aninteger selected from 0 through 1, pa is an integer selected from 0through 6, and W⁷ is selected from the group consisting of O, S, C(O),C(S), C(O)S, C(S)O, C(O)N(R⁷), C(S)N(R⁷), (R⁷)NC(O), (R⁷)NC(S), S(O),S(O)₂, S(O)₂N(R⁷), (R⁷)NS(O)₂, C(NR⁷)N(R⁷), (R⁷)NC(NR⁷), and N(R⁷) withthe proviso that no more than one of the group consisting of rr and pais 0 at the same time; R⁷ and R⁸ are independently selected from thegroup consisting of hydrido, hydroxy, alkyl, and alkoxyalkyl; R¹⁴, R¹⁵,R³⁷, and R³⁸ are independently selected from the group consisting ofhydrido, hydroxy, halo, alkyl, alkoxyalkyl, haloalkyl, haloalkoxy, andhaloalkoxyalkyl; Ψ is selected from the group consisting of NR⁵, O,C(O), C(S), S, S(O), S(O)₂, and CR³⁹R⁴⁰ with the provisos that Ψ isselected from other than NR⁵, O, S, S(O), and S(O)₂ unless any two ofX⁰, R², R¹, and J are other than hydrido, or that Ψ is selected fromother than O, unless A is selected from other than methylene when B isphenyl, that Ψ is selected from other than C(O), unless A is selectedfrom other than methyleneoxy when B is phenyl, or that Ψ is selectedfrom other than NH unless A is selected from other than a singlecovalent bond when B is acyl, or that Ψ is selected from other than NHunless A is selected from other than S(O) or S(O)₂ when B is phenyl; R⁵is selected from the group consisting of hydrido, alkyl, and alkoxy; R³⁹and R⁴⁰ are independently selected from the group consisting of hydrido,hydroxy, halo, hydroxyalkyl, alkyl, alkoxyalkyl, haloalkyl, haloalkoxy,and haloalkoxyalkyl; X⁰, R² and R¹ are independently selected from thegroup consisting of Z⁰-Q, hydrido, alkyl, alkenyl, and halo; X⁰, R² andR¹ are independently selected from the group consisting of amidino,guanidino, dialkyisulfonium, trialkylphosphonium, dialkylsulfoniumalkyl,heteroarylamino, amino, nitro, alkylamino, arylamino, aralkylamino,alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl,haloalkanoyl, hydroxyhaloalkyl, cyano, and phosphono; Z⁰ is selectedfrom the group consisting of covalent single bond, (CR⁴¹R⁴²)_(q) whereinq is an integer selected from 1 through 2,(CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p) wherein g and p are integersindependently selected from 0 through 2 and W⁰ is selected from thegroup consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,C(O)N(R⁴¹), (R⁴¹)NC(O), C(S)N(R⁴¹), (R⁴¹)NC(S), OC(O)N(R⁴¹),(R⁴¹)NC(O)O, SC(S)N(R⁴¹), (R⁴¹)NC(S)S, SC(O)N(R⁴¹), (R⁴¹)NC(O)S,OC(S)N(R⁴¹), (R⁴¹)NC(S)O, N(R⁴²)C(O)N(R⁴¹), (R⁴¹)NC(O)N(R⁴²),N(R⁴²)C(S)N(R⁴¹), (R⁴¹)NC(S)N(R⁴²), S(O), S(O)₂, S(O)₂N(R⁴¹),N(R⁴¹)S(O)₂, N(R⁴¹), ON(R⁴¹), and (CH(R⁴¹))_(e)—W²—(CH(R⁴²))_(h) whereine and h are integers independently selected from 0 through 2 and W² isselected from the group consisting of CR⁴¹═CR⁴², CR⁴¹R⁴²═C; vinylidene),and ethynylidene (C≡C; 1,2-ethynyl), with the provisos that R⁴¹ and R⁴²are selected from other than halo and cyano when directly bonded to Nand Z⁰ is directly bonded to the benzene ring, that W⁰ is selected,wherein g is 0, from other than NHS(O)₂CH₂aryl or N(R⁴¹) unless R⁴¹ isselected from other than hydrido, alkyl, or aralkylsulfonyl, and Z⁰ isselected from other than OC(O), C(O)N(H), and (H)NC(O), unless Q isselected from other than phenyl, 2-furyl, 2-thienyl, 4-thiazolyl,2-pyridyl, 2-naphthyl, 1,2-dihydrobenzofuran-5-yl,1,2-dihydrobenzofuran-6-yl, or 1,2-benzisoxazol-6-yl , or X⁰ is selectedfrom other than hydrido, halo, or methyl, or R¹ is selected from otherthan hydrido, fluoro, hydroxy, acetoxy, propanoyloxy, 2-carboxyacetoxy,2,3 or 4-carboxypropanoyloxy, benzoyloxy, methyl, or methoxy; R⁴¹ andR⁴² are independently selected from the group consisting of hydrido,hydroxy, halo, cyano, aryloxy, hydroxyalkyl, acyl, aroyl, heteroaroyl,heteroaryloxyalkyl, alkoxy, alkyl, aryl, aralkyl, aryloxyalkyl,aralkoxyalkylalkoxy, alkoxyalkyl, heteroaryloxyalkyl, cycloalkyl,cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl,haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy,haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy,halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, saturated heterocyclyl,partially saturated heterocyclyl, heteroaryl, and heteroaralkyl; Q isformula (II):

 wherein D¹, D², J¹, J² and K¹ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, no more than one of D¹, D², J¹, J² andK¹ is O, no more than one of D¹, D², J¹, J² and K¹ is S, one of D¹, D²,J¹, J² and K¹ must be a covalent bond when two of D¹, D², J¹, J² and K¹are O and S, and no more than four of D¹, D², J¹, J² and K¹ are N, withthe proviso that R⁹, R¹⁰, R¹¹, R¹², and R¹³ are each independentlyselected to maintain the tetravalent nature of carbon, trivalent natureof nitrogen, the divalent nature of sulfur, and the divalent nature ofoxygen; Q is selected from the group consisting of alkyl, alkoxy,alkylamino, alkylthio, haloalkylthio, saturated heterocyclyl, alkyl,partially saturated heterocyclyl, acyl, aroyl, heteroaroyl, cycloalkyl,cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, cycloalkylalkenyl,haloalkyl, haloalkoxy, haloalkenyl, halocycloalkyl, halocycloalkenyl,haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxyalkyl, andhalocycloalkenyloxyalkyl; K is (CR^(4a)R^(4b))_(n) wherein n is theinteger 1; R^(4a) and R^(4b) are independently selected from the groupconsisting of halo, hydrido, hydroxy, hydroxyalkyl, alkyl, alkoxyalkyl,and haloalkyl; E⁰ is E¹, when K is (CR^(4a)R^(4b))_(n), wherein E¹ isselected from the group consisting of a covalent single bond, O, S,C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷),(R⁷)NC(S), OC(O)N(R⁷), (R⁷)NC(O)O, SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷),(R⁷)NC(O)S, OC(S)N(R⁷), (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸),N(R⁸)C(S)N(R⁷), (R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂,S(O)₂N(R⁷)C(O), C(O)N(R⁷)S(O)₂, N(R⁷), ON(R⁷), CR^(4a)═CR^(4b),ethynylidene (C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b); K is(CH(R¹⁴))_(j)-T wherein j is selected from a integer from 0 through 1and T is selected from the group consisting of single covalent bond, O,S, and N(R⁷) with the proviso that (CH(R¹⁴))_(j) is bonded to the phenylring; E⁰ is E², when K is (CH(R¹⁴))_(j)-T, wherein E² is selected fromthe group consisting of a covalent single bond, C(O), C(S), C(O)O,C(S)O, C(O)S, C(S)S, C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S),(R⁷)NC(O)O, (R⁷)NC(S)S, (R⁷)NC(O)S, (R⁷)NC(S)O, N(R⁸)C(O)N(R⁷),(R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷), (R⁷)NC(S)N(R⁸), S(O), S(O)₂, S(O)₂N(R⁷),N(R⁷)S(O)₂, S(O)₂N(H)C(O), C(O)N(H)S(O)₂, and N(R⁷); K isG-(CH(R¹⁵))_(k) wherein k is the integer 1 and G is selected from thegroup consisting of O, S, and N(R⁷); E⁰ is E³, when K isG-(CH(R¹⁵))_(k), wherein E³ is selected from the group consisting of acovalent single bond, O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,C(O)N(R⁷), (R⁷)NC(O), C(S)N(R⁷), (R⁷)NC(S), OC(O)N(R⁷), (R⁷)NC(O)O,SC(S)N(R⁷), (R⁷)NC(S)S, SC(O)N(R⁷), (R⁷)NC(O)S, OC(S)N(R⁷), (R⁷)NC(S)O,N(R⁸)C(O)N(R⁷), (R⁷)NC(O)N(R⁸), N(R⁸)C(S)N(R⁷), (R⁷)NC(S)N(R⁸), S(O),S(O)₂, S(O)₂N(R⁷), N(R⁷)S(O)₂, N(R⁷), ON(R⁷), CR^(4a)═CR^(4b),ethynylidene (C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b); Y⁰ is formula(IV):

 wherein D⁵, D⁶, J⁵, and J⁶ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, K² is independently selected from thegroup consisting of C and N⁺, no more than one of D⁵, D⁶, J⁵, and J⁶ isO, no more than one of D⁵, D⁶, J⁵, and J⁶ is S, one of D⁵, D⁶, J⁵, andJ⁶ must be a covalent bond when two of D⁵, D⁶, J⁵, and J⁶ are O and S,no more than three of D⁵, D⁶, J⁵, and J⁶ are N when K² is N⁺, and nomore than four of D⁵, D⁶, J⁵, and J⁶ are N when K² is carbon with theprovisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are each independently selected tomaintain the tetravalent nature of carbon, trivalent nature of nitrogen,the divalent nature of sulfur, and the divalent nature of oxygen; Q^(b)is selected from the group consisting of NR²⁰R²¹, ⁺NR²⁰R²¹R²², oxy,alkyl, alkylaminoalkyl, aminoalkyl, dialkylsulfoniumalkyl, and acylaminowherein R²⁰, R²¹, and R²² are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino,aminoalkyl, and hydroxyalkyl with the provisos that no more than one ofR²⁰, R²¹, and R²² is hydroxy, alkoxy, alkylamino, amino, or dialkylaminoand that R²⁰, R²¹, and R²² must be other than be hydroxy, alkoxy,alkylamino, amino, and dialkylamino when K² is N⁺; Q^(b) is selectedfrom the group consisting of N(R²⁶)SO²N(R²³)(R²⁴), N(R²⁶)C(O)OR⁵,N(R²⁶)C(O)SR⁵, N(R²⁶)C(S)OR⁵ and N(R²⁶)C(S)SR⁵ with the proviso that nomore than one of R²³, R²⁴, and R²⁶ is hydroxy, alkoxy, alkylamino,amino, or dialkylamino when two of the group consisting of R²³, R²⁴, andR²⁶ are bonded to the same atom; Q^(b) is selected from the groupconsisting of dialkylsulfonium, trialkylphosphonium, C(NR²⁵)NR²³R²⁴,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)C(O)N(R²³)(R²⁴), N(R²⁶)C(S)N(R²³)(R²⁴),C(NR²⁵)OR⁵, C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(S)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO²N(R²³)(R²⁴), C(NR²⁵)SR⁵,C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with the provisos that no more than one ofR²³, R²⁴, and R²⁶ is hydroxy, alkoxy, alkylamino, amino, or dialkylaminowhen two of the group consisting of R²³, R²⁴, and R²⁶ are bonded to thesame atom and that said Q^(b) group is bonded directly to a carbon atom;R²³, R²⁴, R²⁵, and R²⁶ are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino,aminoalkyl, and hydroxyalkyl; Q^(s) is selected from the groupconsisting of a single covalent bond, (CR³⁷R³⁸)_(b)—(W⁰)_(az) wherein azis an integer selected from 0 through 1, b is an integer selected from 1through 2, and W⁰ is selected from the group consisting of O, S, C(O),C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴),(R¹⁴)NC(S), OC(O)N(R¹⁴), SC(S)N(R¹⁴), SC(O)N(R¹⁴), OC(S)N(R¹⁴),N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵),S(O), S(O)₂, S(O)₂N(R¹⁴), N(R¹⁴)(O)₂, N(R¹⁴), ON(R¹⁴),(CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 2, and W¹ is selected from thegroup consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,C(O)N(R¹⁴), (R¹⁴)NC(O), C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴),(R¹⁴)NC(O)O, SC(S)N(R¹⁴), (R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S,OC(S)N(R¹⁴), (R¹⁴)NC(S)O, N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵),N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵), S(O), S(O)₂, S(O)₂N(R¹⁴),N(R¹⁴)S(O)₂, N(R¹⁴), ON(R¹⁴), and (CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) whereine and h are integers independently selected from 0 through 2 and W² isselected from the group consisting of CR^(4a)═CR^(4b), ethynylidene(C≡C; 1,2-ethynyl), and C═CR^(4a)R^(4b) with the provisos that R¹⁴ andR¹⁵ are selected from other than halo and cyano when directly bonded toN and that (CR³⁷R³⁸)_(b), (CH(R¹⁴))_(c), (CH(R¹⁴))_(e) and are bonded toE⁰; Y⁰ is Q^(b)-Q^(ss) wherein Q^(ss) is selected from the groupconsisting of (CR³⁷R⁷)_(f) wherein f is an integer selected from 1through 4, (CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 2, and W¹ is selected from thegroup consisting of W¹ is selected from the group consisting of O, S,C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R¹⁴), (R¹⁴)NC(O),C(S)N(R¹⁴), (R¹⁴)NC(S), OC(O)N(R¹⁴), (R¹⁴)NC(O)O, SC(S)N(R¹⁴),(R¹⁴)NC(S)S, SC(O)N(R¹⁴), (R¹⁴)NC(O)S, OC(S)N(R¹⁴), (R¹⁴)NC(S)O,N(R¹⁵)C(O)N(R¹⁴), (R¹⁴)NC(O)N(R¹⁵), N(R¹⁵)C(S)N(R¹⁴), (R¹⁴)NC(S)N(R¹⁵),S(O), S(O)₂, S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, N(R¹⁴), ON(R¹⁴), and(CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h) wherein e and h are integersindependently selected from 0 through 2 and W² is selected from thegroup consisting of CR^(4a)═CR^(4b), ethynylidene (C≡C; 1,2-ethynyl),and C═CR^(4a)R^(4b) with the provisos that R¹⁴ and R¹⁵ are selected fromother than halo when directly bonded to N and that (CR³⁷R³⁸)_(f),(CH(R¹⁵))_(c), and (CH(R¹⁵))_(e) are bonded to E⁰; Y⁰ is Q^(b)-Q^(sss)wherein QQ^(sss) is (CH(R³⁸))_(r)—W³, r is an integer selected from 1through 2, and W³ is selected from the group consisting of1,1-cyclopropyl, 1,2-cyclopropyl, 1,1-cyclobutyl, 1,2-cyclobutyl,1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl,1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl,2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl,1,3-piperazinyl, 1,4-piperazinyl, 2,3-piperazinyl, 2,5-piperazinyl,2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 1,4-piperidinyl,2,3-piperidinyl, 2,4-piperidinyl, 2,5-piperidinyl, 2,6-piperidinyl,3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl, 1,2-pyrrolidinyl,1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl,3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl, 2H-2,5-pyranyl,4H-2,3-pyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl,2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl,2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl,2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl,2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and 3,5-tetrahydropyranylwith the proviso that (CH(R³⁸))_(r) is bonded to E⁰ and Q^(b) is bondedto lowest numbered substituent position of each W³; Y⁰ is Q^(b)-Q^(sssr)wherein Q^(sssr) is (CH(R³⁸))_(r)—W⁴, r is an integer selected from 1through 2, and W⁴ is selected from the group consisting of1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl,1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl,2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl,1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl, 2,3-piperazinyl,2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl,1,4-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,5-piperidinyl,2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl,1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl,2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl,2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl,2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl,2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl,3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl, 2,4-tetrahydrofuranyl,2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and3,5-tetrahydropyranyl with the provisos that (CH(R³⁸))_(r) is bonded toE⁰ and Q^(b) is bonded to highest number substituent position of eachW⁴; Y⁰ is Q^(b)-Q^(ssss) wherein Q^(ssss) is (CH(R³⁸))_(r)—W⁵, r is aninteger selected from 1 through 2, and W⁵ is selected from the groupconsisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl,2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl,3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl,2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl,3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to lowest number substituent position of each W⁵ andthat (CH(R³⁸))_(r) is bonded to E⁰; Y⁰ is Q^(b)-Q^(ssssr) whereinQ^(ssssr) is (CH(R³⁸))_(r)—W⁶, r is an integer selected from 1 through2, and W⁶ is selected from the group consisting of 1,4-indenyl,1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl,2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl,3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl,2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl,3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl,2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl,3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl,2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl,3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl,1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl,2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl,3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl,2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl,3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl,1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl,2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl,2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl,2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl,3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl,4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl,1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl,3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl,3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl,4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl,3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl,4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl withthe proviso that Q^(b) is bonded to highest number substituent positionof each W⁶ and that (CH(R³⁸))_(r) is bonded to E⁰.
 4. The compound asrecited in claim 3 or a pharmaceutically acceptable salt thereof,wherein; J is selected from the group consisting of hydrido, halo,hydroxy, hydroxyalkyl, amino, aminoalkyl, O—R⁶, NH—R⁶, and S—R⁶, whereinR⁶ is selected from the group consisting of alkyl and haloalkkyl; B isformula (V):

 wherein D¹, D², J¹, J² and K¹ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, no more than one of D¹, D², J¹, J² andK¹ is O, no more than one of D¹, D², J¹, J² and K¹ is S, one of D¹, D²,J¹, J² and K¹ must be a covalent bond when two of D¹, D², J¹, J² and K¹are O and S, and no more than four of D¹, D², J¹, J² and K¹ are N; R³²,R³³, R³⁴, R³⁵, and R³⁶ are independently selected to be Q^(b); R⁹, R¹⁰,R¹¹, R¹², R¹³, R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selectedfrom the group consisting of hydrido, amidino, guanidino,dialkylsulfonium, carboxy, haloalkylthio, alkanoyloxy, alkoxy,alkoxyalkyl, haloalkoxylalkyl, hydroxy, amino, alkoxyamino, thio, nitro,lower alkylamino, alkylthio, alkylthioalkyl, alkylsulfinyl,alkylsulfinylalkyl, alkylsulfonyl, alkylsulfonylalkyl,haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido,alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkylamidosulfonyl, monoarylamidosulfonyl, alkanoyl, alkenoyl, haloalkanoyl,alkyl, alkenyl, alkenyloxy, alkenyloxyalky, halo, haloalkyl,haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl,haloalkoxyalkyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido,alkylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl,carboxamido, carboxamidoalkyl, and cyano; B is selected from the groupconsisting of C3-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, C3-C8haloalkyl, and C3-C8 haloalkenyl wherein each member of group B may beoptionally substituted at any carbon up to and including 6 atoms fromthe point of attachment of B to A with one or more of the groupconsisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆; B is selected from the groupconsisting of C3-C10 cycloalkyl, C5-C10 cycloalkenyl, C4-C9 saturatedheterocyclyl, and C4-C9 partially saturated heterocyclyl, wherein eachring carbon may be optionally substituted with R₃₃, a ring carbon otherthan the ring carbon at the point of attachment of B to A may beoptionally substituted with oxo provided that no more than one ringcarbon is substituted by oxo at the same time, ring carbon and nitrogenatoms adjacent to the carbon atom at the point of attachment may beoptionally substituted with R₉ or R₁₃, a ring carbon or nitrogen atomadjacent to the R₉ position and two atoms from the point of attachmentmay be substituted with R₁₀, a ring carbon or nitrogen atom adjacent tothe R₁₃ position and two atoms from the point of attachment may besubstituted with R₁₂, a ring carbon or nitrogen atom three atoms fromthe point of attachment and adjacent to the R₁₀ position may besubstituted with R₁₁, a ring carbon or nitrogen atom three atoms fromthe point of attachment and adjacent to the R₁₂ position may besubstituted with R₃₃, and a ring carbon or nitrogen atom four atoms fromthe point of attachment and adjacent to the R₁₁ and R₃₃ positions may besubstituted with R₃₄; A is selected from the group consisting of singlecovalent bond, (W⁷)_(rr)—(CH(R¹⁵))_(pa) and (CH(R¹⁵))_(pa)—(W⁷)_(rr)wherein rr is an integer selected from 0 through 1, pa is an integerselected from 0 through 6, and W⁷ is selected from the group consistingof O, S, C(O), C(S), C(O)S, C(S)O, C(O)N(R⁷), C(S)N(R⁷), (R⁷)NC(O),(R⁷)NC(S), S(O), S(O)₂, S(O)₂N(R⁷), (R⁷)NS(O)₂, C(NR⁷)N(R⁷),(R⁷)NC(NR⁷), and N(R⁷) with the proviso that no more than one of thegroup consisting of rr and pa is 0 at the same time; R⁷ and R⁸ areindependently selected from the group consisting of hydrido, hydroxy,alkyl, and alkoxyalkyl; R¹⁵ is selected from the group consisting ofhydrido, hydroxy, halo, alkyl, and haloalkyl; Ψ is NH with the provisosthat Ψ is selected from other than NH unless any two of X⁰, R², R¹, andJ are other than hydrido or that Ψ is selected from other than NH unlessA is selected from other than a single covalent bond when B is acyl, orthat Ψ is selected from other than NH unless A is selected from otherthan S(O) or S(O)₂ when B is phenyl; X⁰ is hydrido; R¹ is selected fromthe group consisting of hydrido, alkyl, alkoxy, alkylamino, alkylthio,haloalkylthio, haloalkyl, haloalkoxy, and halo; R² is selected from thegroup consisting of Z⁰-Q, hydrido, alkyl, alkenyl, and halo; Z⁰ is acovalent single bond; Q is formula (II):

 wherein D¹, D², J¹, J² and K¹ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, no more than one of D¹, D², J¹, J² andK¹ is O, no more than one of D¹, D², J¹, J² and K¹ is S, one of D¹, D²,J¹, J² and K¹ must be a covalent bond when two of D¹, D², J¹, J² and K¹are O and S, and no more than four of D¹, D², J¹, J² and K¹ are N, withthe proviso that R⁹, R¹⁰, R¹¹, R¹², and R¹³ are each independentlyselected to maintain the tetravalent nature of carbon, trivalent natureof nitrogen, the divalent nature of sulfur, and the divalent nature ofoxygen; K is CR^(4a)R^(4b); R^(4a) and R^(4b) are independently selectedfrom the group consisting of halo, hydrido, hydroxy, alkyl, andhaloalkyl; E⁰ is E¹, when K is CR^(4a)R^(4b), wherein E¹ is selectedfrom the group consisting of a covalent single bond, C(O)N(H), (H)NC(O),C(S)N(H), (H)NC(S), S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), andC(O)N(H)S(O)₂; K is (CH(R¹⁴))_(j)-T wherein j is selected from aninteger from 0 through 1 and T is selected from the group consisting ofsingle covalent bond and N(R⁷) with the proviso that (CH(R¹⁴))_(j) isbonded to the phenyl ring; E⁰ is E², when K is (CH(R¹⁴))_(j)-T, whereinE² is selected from the group consisting of C(O)N(H), (H)NC(O),C(S)N(H), (H)NC(S), S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), andC(O)N(H)S(O)₂; R¹⁴ is selected from the group consisting of hydrido,halo, alkyl, and haloalkyl; Y⁰ is formula (IV):

 wherein D⁵, D⁶, J⁵, and J⁶ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, K² is independently selected from thegroup consisting of C and N⁺, no more than one of D⁵, D⁶, J⁵, and J⁶ isO, no more than one of D⁵, D⁶, J⁵, and J⁶ is S, one of D⁵, D⁶, J⁵, andJ⁶ must be a covalent bond when two of D⁵, D⁶, J⁵, and J⁶ are O and S,no more than three of D⁵, D⁶, J⁵, and J⁶ are N when K² is N⁺, and nomore than four of D⁵, D⁶, J⁵, and J⁶ are N when K² is carbon with theprovisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are each independently selected tomaintain the tetravalent nature of carbon, trivalent nature of nitrogen,the divalent nature of sulfur, and the divalent nature of oxygen; R¹⁶,R¹⁷, R¹⁸, and R¹⁹ are independently selected from the group consistingof hydrido, amidino, guanidino, dialkylsulfonium, carboxy,haloalkylthio, alkoxy, hydroxy, amino, thio, nitro, lower alkylamino,alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, alkenoyl,haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboalkoxy,carboalkoxyalkyl, and cyano; Q^(b) is selected from the group consistingof NR²⁰R²¹, ⁺NR²⁰R²¹R²², oxy, alkyl, alkylaminoalkyl, aminoalkyl,dialkylsulfoniumalkyl, and acylamino wherein R²⁰, R²¹, and R²² areindependently selected from the group consisting of hydrido, alkyl,hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkylwith the provisos that no more than one of R²⁰, R²¹, and R²² is hydroxy,alkoxy, alkylamino, amino, or dialkylamino and that R²⁰, R²¹, and R²²must be other than be hydroxy, alkoxy, alkylamino, amino, ordialkylamino when K² is N⁺; Q^(b) is N(R²⁶)SO²N(R²³)(R²⁴) with theproviso that no more than one of R²³, R²⁴, and R²⁶ is hydroxy, alkoxy,alkyl amino, amino, or dialkylamino when two of the group consisting ofR²³, R²⁴, and R²⁶ are bonded to the same atom; Q^(b) is selected fromthe group consisting of dialkylsulfonium, trialkylphosphonium,C(NR²⁵)NR²³R²⁴, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)C(O)N(R²³)(R²⁴),N(R²⁶)C(S)N(R²³)(R²⁴), C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),C(S)N(R²⁶)C(NR²⁶)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with theprovisos that no more than one of R²³, R²⁴, and R²⁶ is hydroxy, alkoxy,alkylamino, amino, or dialkylamino when two of the group consisting ofR²³, R²⁴, and R²⁶ are bonded to the same atom and that said Q^(b) groupis bonded directly to a carbon atom; R²³, R²⁴, R²⁵, and R²⁶ areindependently selected from the group consisting of hydrido, alkyl,hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl;Q^(s) is selected from the group consisting of a single covalent bondand (CR³⁷R³⁸)_(b)—(W⁰)_(az) wherein az is an integer selected from 0through 1, b is an integer selected from 1 through 2, and W⁰ is selectedfrom the group consisting of O, S, C(O), S(O)₂, N(R¹⁴), and ON(R¹⁴) withthe proviso that R¹⁴ is selected from other than halo when directlybonded to N and that (CR³⁷R³⁸)_(b) is bonded to E⁰; R³⁷ and R³⁸ areindependently selected from the group consisting of hydrido, halo,alkyl, and haloalkyl; Y⁰ is Q^(b)-Q^(sss) wherein Q^(ssss) is(CH(R³⁸))_(r)—W⁵, r is an integer selected from 1 through 2, and W⁵ isselected from the group consisting of 1,4-indenyl, 1,5-indenyl,1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl,2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl,2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl,3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl,2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl,2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl,3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl,2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl,3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl,2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl,1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl,3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl,2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl,3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl,1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl,2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to lowest number substituent position of each W⁵ andthat (CH(R³⁸))_(r) is bonded to E⁰; Y⁰ is Q^(b)-Q^(sssr) whereinQ^(ssssr) is (CR(R³⁸))_(r)—W⁶, r is an integer selected from 1 through2, and W⁶ is selected from the group consisting of 1,4-indenyl,1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl,2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl,3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl,2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl,3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl,2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl,3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl,2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl,3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl,1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl,2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl,3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl,2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl,1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl,2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl,2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl,3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl,3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl,4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl,1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl,3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl,3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl,4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl,3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl,4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso thatQ^(b) is bonded to highest number substituent position of each W⁶ andthat (CH(R³⁸))_(r) is bonded to E⁰.
 5. The compound as recited in claim4 having the Formula I-S:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of fluoro, chloro, bromo, hydroxy,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, amino, aminomethyl,1-aminoethyl, 2-aminoethyl, methoxy, ethoxy, trifluoromethoxy,N-methylamino, N-ethylamino, methythio, ethylthio, andtrifluoromethylthio; B is selected from the group consisting of phenyl,2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl,2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl,1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, 1,2,4-oxadiazol-3-yl,1,2,4-oxadiazol-5-yl, 1,3,4-oxadiazol-3-yl, 1,3,4-oxadiazol-5-yl,3-isothiazolyl, 5-isothiazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl,5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl,2-pyrimidinyl, 4-pyrimidinyl, 5-pryimidinyl, 3-pyridazinyl,4-pyridazinyl, 1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl,1,2,4-triazin-5-yl, 1,2,4-triazin-6-yl, and 1,2,3-triazin-4-yl, whereina carbon adjacent to the carbon at the point of attachment may besubstituted by R³², the other carbon adjacent to the carbon at the pointof attachment may be substituted by R³⁶, a carbon adjacent to R³² andtwo atoms from the carbon at the point of attachment may be substitutedby R³³, a carbon adjacent to R³⁶ and two atoms from the carbon at thepoint of attachment may be substituted by R³⁵, and any carbon adjacentto both R³³ and R³⁵ may be substituted by R³⁴; R³², R³³, R³⁴, R³⁵, andR³⁶ are independently selected from the group consisting of hydrido,amidino, guanidino, dimethylsulfonium, carboxy, methoxy, ethoxy,isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, thio,nitro, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-methylamino,dimethylamino, N-ethylamino, methyltilo, ethylthio, isopropylthio,trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl,ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl, propanoyl,trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl,2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, cyano, and Q^(b); B is selected from thegroup consisting of 1-propenyl, propyl, isopropyl, butyl, 2-butenyl,3-butenyl, 2-butynyl, sec-butyl, isobutyl, 2-methylpropenyl, 1-pentyl,2-pentenyl, 3-pentenyl, 4-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl,1-methyl-2-butenyl, 1-methyl-3-butenyl, 1-methyl-2-butynyl, 3-pentyl,1-ethyl-2-propenyl, 2-methylbutyl, 2-methyl-2-butenyl,2-methyl-3-butenyl, 2-methyl-3-butynyl, 3-methylbutyl,3-methyl-2-butenyl, 3-methyl-3-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl,4-hexenyl, 5-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl,1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl,1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl,1-ethyl-3-butenyl, 1-propyl-2-propenyl, 1-ethyl-2-butynyl, 1-heptyl,2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 2-heptynyl,3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl,1-methyl-3-hexenyl, 1-methyl-4-hexenyl, 1-methyl-5-hexenyl,1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl,1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-4-pentenyl,1-butyl-2-propenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 1-octyl,2-octenyl, 3-octenyl, 4-octenyl, 5-octenyl, 6-octenyl, 7-octenyl,2-octynyl, 3-octynyl, 4-octynyl, 5-octynyl, 6-octynyl, 2-octyl,1-methyl-2-heptenyl, 1-methyl-3-heptenyl, 1-methyl-4-heptenyl,1-methyl-5-heptenyl, 1-methyl-6-heptenyl, 1-methyl-2-heptynyl,1-methyl-3-heptynyl, 1-methyl-4-heptenyl, 1-methyl-5-heptenyl,1-methyl-6-heptenyl, 1-methyl-2-heptenyl, 1-methyl-3-heptynyl,1-methyl-4-heptynyl, 1-methyl-5-heptynyl, 3-octyl, 1-ethyl-2-hexenyl,1-ethyl-3-hexenyl, 1-ethyl-4-hexenyl, 1-ethyl-2-hexynyl,1-ethyl-3-hexynyl, 1-ethyl-4-hexynyl, 1-ethyl-5-hexenyl,1-pentyl-2-propenyl, 4-octyl, 1-propyl-2-pentenyl, 1-propyl-3-pentenyl,1-propyl-4-pentenyl, 1-butyl-2-butenyl, 1-propyl-2-pentynyl,1-propyl-3-pentynyl, 1-butyl-2-butnyl, 1-butyl-3-butenyl,2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl,4-trifluoromethylpentyl, 5,5,6,6,6-pentafluoroheyyl, and3,3,3-trifluoropropyl, wherein each member of group B may be optionallysubstituted at any carbon up to and including 5 atoms from the point ofattachment of B to A with one or more of the group consisting of R₃₂,R₃₃, R₃₄, R₃₅, and R₃₆; B is selected from the group consisting ofcyclopropyl, cyclobutyl, oxetan-2-yl, oxetan-3-yl, azetidin-1-yl,azetidin-2-yl, azetidin-3-yl, thiaetan-2-yl, thiaetan-3-yl, cyclopentyl,cyclopent-2-enyl, cyclopent-3-enyl, cyclohexyl, 4-methylcyclohexyl,4-chloro-3-ethylphenoxycyclohexyl, 3-trifluoromethoxyphenoxycyclohexyl,3-trifluoromethylcyclohexyl, 4-trifluoromethylcyclohexyl,3,5-bis-trifluoromethylcyclohexyl, adamantyl,3-trifluoromethyladamantyl, norbornyl, 3-trifluoromethylnorbornyl,norbornenyl, 7-oxabicyclo[2.2.1]heptan-2-yl, bicyclo[3.1.0]hexanyl,cyclohex-2-enyl, cyclohex-3-enyl, cycloheptyl, cyclohept-2-enyl,cyclohept-3-enyl, cyclooctyl, cyclooct-2-enyl, cyclooct-3-enyl,cyclooct-4-enyl, 2-morpholinyl, 3-morpholinyl, 4-morpholinyl,1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl,3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl,3-pyrrolidinyl, 2-dioxanyl, 2H-2-pyranyl, 2H-3-pyranyl, 2H-4-pyranyl,4H-2-pyranyl, 4H-3-pyranyl, 4H-4-pyranyl, 2H-pyran-2-one-3-yl,2H-pyran-2-one-4-yl, 2H-pyran-2-one-5-yl, 4H-pyran-4-one-2-yl,4H-pyran4-one-3-yl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl,2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl,2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein each ring carbonmay be optionally substituted with R₃₃, a ring carbon and nitrogen atomsadjacent to the carbon atom at the point of attachment may be optionallysubstituted with R₉ or R₁₃, a ring carbon or nitrogen atom adjacent tothe R₉ position and two atoms from the point of attachment may besubstituted with R₁₀, and a ring carbon or nitrogen atom adjacent to theR₁₃ position and two atoms from the point of attachment may besubstituted with R₁₂; R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independentlyselected from the group consisting of amidino, guanidino,dimethylsulfonium, methylethylsulfonium, carboxy, methoxy, ethoxy,isopropoxy, propoxy, butoxy, hydroxy, amino, methoxyamino, ethoxyamino,aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-dimethylamino,N-methylamino, N-ethylamino, methylsulfinyl, ethylsulfinyl,methylsulfonyl, ethylsulfonyl, amidosulfonyl, N-methylamidosulfonyl,N,N-dimethylamidosulfonyl, acetyl, propanoyl, butanoyl, trifluoroacetyl,pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,2-carboxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl,N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano; A isselected from the group consisting of single covalent bond, O, C(O),CH₂, CH₃CH, CF₃CH, CH₃CC(O), CF₃CC(O), C(O)CCH₃, C(O)CCF₃, CH₂C(O),(O)CCH₂, CH₂CH₂, CH₂CH₂CH₂, CH₃CCH₂, CF₃CCH₂, CH₃CC(O)CH₂, CF₃CC(O)CH₂,CH₂C(O)CCH₃, CH₂C(O)CCF₃, CH₂CH₂C(O), and CH₂(O)CCH₂; R¹ is selectedfrom the group consisting of hydrido, methyl, ethyl, propyl, butyl,methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butoxy, N-methylamino, N,N-dimethylamino, N-ethyl amino, N,N-diethylamino, methylthio,ethylthio, isopropylthio, trifluoromethylthio, trifuoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl,trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;R² is selected from the group consisting of phenyl, 2-thienyl,3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl,4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 1,2,4-triazol-3-yl,1,2,4-triazol-5-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl,1,3,4-oxadiazol-3-yl, 1,3,4-oxadiazol-5-yl, 3-isothiazolyl,5-isothiazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl,2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl,4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl,1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl,1,2,4-triazin-6-yl, and 1,2,3-triazin-4-yl, wherein a carbon adjacent tothe carbon at the point of attachment may be substituted by R⁹, theother carbon adjacent to the carbon at the point of attachment may besubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment may be substituted by R¹⁰, a carbonadjacent to R¹³ and two atoms from the carbon at the point of attachmentmay be substituted by R¹², and any carbon adjacent to both R¹⁰ and R¹²may be substituted by R¹¹; K is CR^(4a)R^(4b) wherein R^(4a) and R^(4b)are independently selected from the group consisting of chloro, fluoro,and hydrido; E⁰ is E¹, when K is CR^(4a)R^(4b), wherein E¹ is selectedfrom the group consisting of a covalent single bond, C(O)N(H), (H)NC(O),S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂; K is selectedfrom the group consisting of N(H) and CH₂N(H); E⁰ is E², when K is N(H)and CH₂N(H), wherein E² is selected from the group consisting ofC(O)N(H), (H)NC(O), S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), andC(O)N(H)S(O)₂; Y⁰ is selected from the group of formulas consisting of:

R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, dimethylsulfoniumn, carboxy,methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino,ethoxyamino, thio, nitro, aminomethyl, 1-aminoethyl, 2-aminoethyl,N-N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio,isopropylthio, trifluoromethylthio, methyl sulfinyl, ethyl sulfinyl,methyl sulfonyl, ethyl sulfonyl, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl, propanoyl,trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl,2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano; Q^(b) is selected, when bonded toa carbon, from the group consisting of NR²⁰R²¹, ⁺NR²⁰R²¹R²²,dimethylsulfonium, methylethylsulfonium, diethylsulfonium,trimethylphosphonium, C(NR²⁵)NR²³R²⁴, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with theprovisos that no more than one of R²⁰, R²¹, and R²² is hydroxy, methoxy,ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino, or aminoand that no more than one of R²³, R²⁴, and R²⁶ is hydroxy, methoxy,ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino, or aminowhen two of the group consisting of R²³, R²⁴, and R²⁶ are bonded to thesame atom and that said Q^(b) group is bonded directly to a carbon atom;R²⁰, R²¹, R²², R²³, R²⁴, R²⁵, and R²⁶ are independently selected fromthe group consisting of hydrido, methyl, ethyl, propyl, butyl,isopropyl, hydroxy, methoxy, ethoxy, isopropoxy, propoxy, 2-aminoethyl,2-(N-methylamino)ethyl, 2-(N,N-dimethylamino)ethyl,2-(N,N,N-trimethylamino)ethyl, N-(2-hydroxyethyl)amino,N,N-bis-(2-hydroxyethyl)amino, N-(2-hydroxyethyl)-N-(2-aminoethyl)amino,N-methylamino, N-ethylamino, N,N-dimethylamino, N,N-diethylamino, andN,N,N-trimethylamino; Q^(b) is selected, when bonded to a nitrogen, fromthe group consisting of oxy, methyl, ethyl, 2-aminoethyl,2-(N-methylamino)ethyl, 2-(N,N-dimethylamino)ethyl,2-(N,N,N-trimethylamino)ethyl, N-(2-hydroxyethyl)amino,N,N-bis-(2-hydroxyethyl)amino, amino, hydroxylamino, N-methoxyamino,N-methylamino, N,N-dimethylamino, and N,N,N-trimethylamino; Q^(s) isselected from the group consisting of a single covalent bond, CH₂,CH₃CH, CF₂, CF₃CH, CH₂O, CH₃C(H)O, CF₃C(H)O, CH₂S, CH₃C(H)S, CF₃C(H)S,CH₂C(O), CH₃C(H)C(O), CF₃C(H)C(O), and CF₂C(O) with the proviso thatQ^(s) is bonded to E⁰ through a carbon atom.
 6. The compound as recitedin claim 1 or a pharmaceutically acceptable salt thereof, wherein; J isselected from the group consisting of halo, hydroxy, hydroxyalkyl,amino, aminoalkyl, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ is selected fromthe group consisting of alkyl and haloalkyl; B is selected from thegroup consisting of aryl and heteroaryl wherein a carbon adjacent to thecarbon at the point of attachment may be substituted by R³², the othercarbon adjacent to the carbon at the point of attachment may besubstituted by R³⁶, a carbon adjacent to R³² and two atoms from thecarbon at the point of attachment may be substituted by R³³, a carbonadjacent to R³⁶ and two atoms from the carbon at the point of attachmentmay be substituted by R³⁵, and any carbon adjacent to both R³³ and R³⁵may be substituted by R³⁴; R³², R³³, R³⁴, R³⁵, and R³⁶ are independentlyselected from the group consisting of hydrido, amidino, guanidino,dialkylsulfonium, carboxy, haloalkylthio, alkoxy, hydroxy, amino,alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylsulfinyl,alkylsulfonyl, amidosulfonyl, alkanoyl, haloalkanoyl, alkyl, halo,haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl,aminoalkyl, carboxyalkyl, carboalkoxy, carboxamido, cyano, and Q^(b); Bis selected from the group consisting of C3-C8 alkyl, C3-C8 alkenyl,C3-C8 haloalkyl, and C3-C8 haloalkenyl wherein each member of group Bmay be optionally substituted at any carbon up to and including 6 atomsfrom the point of attachment of B to A with one or more of the groupconsisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆; B is selected from the groupconsisting of C3-C10 cycloalkyl, C5-C10 cycloalkenyl, C4-C9 saturatedheterocyclyl, and C4-C9 partially saturated heterocyclyl, wherein eachring carbon may be optionally substituted with R₃₃, a ring carbon otherthan the ring carbon at the point of attachment of B to A may beoptionally substituted with oxo provided that no more than one ringcarbon is substituted by oxo at the same time, ring carbon and nitrogenatoms adjacent to the carbon atom at the point of attachment may beoptionally substituted with R₉ or R₁₃, a ring carbon or nitrogen atomadjacent to the R₉ position and two atoms from the point of attachmentmay be substituted with R₁₀, a ring carbon or nitrogen atom adjacent tothe R₁₃ position and two atoms from the point of attachment may besubstituted with R₁₂, a ring carbon or nitrogen atom three atoms fromthe point of attachment and adjacent to the R₁₀ position may besubstituted with R₁₁, a ring carbon or nitrogen atom three atoms fromthe point of attachment and adjacent to the R₁₂ position may besubstituted with R₃₃, and a ring carbon or nitrogen atom four atoms fromthe point of attachment and adjacent to the R₁₁ and R₃₃ positions may besubstituted with R₃₄; R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independentlyselected from the group consisting of hydrido, amidino, guanidino,dialkylsulfonium, carboxy, haloalkylthio, alkoxy, hydroxy, amino,alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylsulfinyl,alkylsulfonyl, amidosulfonyl, alkanoyl, haloalkanoyl, alkyl, halo,haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl,aminoalkyl, carboxyalkyl, carboalkoxy, carboxamido, and cyano; A isselected from the group consisting of single covalent bond,(W⁷)_(rr)—(CH(R¹⁵))_(pa) and (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is aninteger selected from 0 through 1, pa is an integer selected from 0through 6, and W⁷ is selected from the group consisting of O, S, andC(O) with the proviso that no more than one of the group consisting ofrr and pa is the integer 0 at the same time; R¹⁵ is selected from thegroup consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl; Ψ isNH; X⁰ is hydrido; R¹ is selected from the group consisting of hydrido,alkyl, alkoxy, alkylamino, alkylthio, haloalkylthio, haloalkyl,haloalkoxy, and halo; R² is Q, wherein Q is selected from the groupconsisting of aryl and heteroaryl wherein a carbon adjacent to thecarbon at the point of attachment may be substituted by R⁹, the othercarbon adjacent to the carbon at the point of attachment may besubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment may be substituted by R¹⁰, a carbonadjacent to R¹³ and two atoms from the carbon at the point of attachmentmay be substituted by R¹², and any carbon adjacent to both R¹⁰ and R¹²may be substituted by R¹¹; K is CR^(4a)R^(4b) wherein R^(4a) and R^(4b)are independently selected from the group consisting of halo andhydrido; E⁰ is E¹, when K is CR^(4a)R^(4b), wherein E¹ is selected fromthe group consisting of a covalent single bond, C(O)N(H), (H)NC(O),S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂; K is(CH(R¹⁴))_(j)-T wherein j is selected from an integer from 0 through 1and T is selected from the group consisting of single covalent bond andN(R⁷) with the proviso that (CH(R¹⁴))_(j) is bonded to the phenyl ring;R⁷ is selected from the group consisting of hydrido, hydroxy, alkyl, andalkoxyalkyl; R¹⁴ is selected from the group consisting of hydrido andhalo; E⁰ is E², when K is (CH(R¹⁴))_(j)-T, wherein E² is selected fromthe group consisting of C(O)N(H), (H)NC(O), S(O)₂N(H), N(H)S(O)₂,S(O)₂N(H)C(O), and C(O)N(H)S(O)₂; Y⁰ is formula (IV):

 wherein D⁵, D⁶, J⁵ and J⁶ are independently selected from the groupconsisting of C, N, O, S and a covalent bond with the provisos that nomore than one is a covalent bond, K² is independently selected from thegroup consisting of C and N⁺, no more than one of D⁵, D⁶, J⁵, and J⁶ isO, no more than one of D⁵, D⁶, J⁵, and J⁶ is S, one of D⁵, D⁶, J⁵, andJ⁶ must be a covalent bond when two of D⁵, D⁶, J⁵, and J⁶ are O and S,no more than three of D⁵, D⁶, J⁵, and J⁶ are N when K² is N⁺, and nomore than four of D⁵, D⁶, J⁵, and J⁶ are N when K² is carbon with theprovisos that R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are each independently selected tomaintain the tetravalent nature of carbon, trivalent nature of nitrogen,the divalent nature of sulfur, and the divalent nature of oxygen; R¹⁶,R¹⁷, R¹⁸, and R¹⁹ are independently selected from the group consistingof hydrido, amidino, guanidino, dialkylsulfonium, carboxy,haloalkylthio, alkoxy, hydroxy, amino, thio, nitro, lower alkylamino,alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, alkenoyl,haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboalkoxy,carboalkoxyalkyl, and cyano; Q^(b) is selected from the group consistingof NR²⁰R²¹, ⁺NR²⁰R²¹R²², oxy, alkyl, alkylaminoalkyl, aminoalkyl,dialkylsulfoniumalkyl, and acylamino wherein R²⁰, R²¹, and R²² areindependently selected from the group consisting of hydrido, alkyl,hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkylwith the provisos that no more than one of R²⁰, R²¹, and R²² is hydroxy,alkoxy, alkylamino, amino, or dialkylamino and that R²⁰, R²¹, and R²²must be other than be hydroxy, alkoxy, alkylamino, amino, ordialkylamino when K² is N⁺; Q^(b) is selected from the group consistingof dialkylsulfonium, trialkylphosphonium, C(NR²⁵)NR²³R²⁴,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴,and C(O)NR²³R²⁴ with the provisos that no more than one of R²³, R²⁴, andR²⁶ is hydroxy, alkoxy, alkylamino, amino, or dialkylamino when two ofthe group consisting of R²³, R²⁴, and R²⁶ are bonded to the same atomand that said Q^(b) group is bonded directly to a carbon atom; R²³, R²⁴,R²⁵, and R²⁶ are independently selected from the group consisting ofhydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl,and hydroxyalkyl; Q^(s) is selected from the group consisting of asingle covalent bond and (CR³⁷R³⁸)_(b) 13 (W⁰)_(az) wherein az is aninteger selected from 0 through 1, b is the integer 1, and W⁰ isselected from the group consisting of O, S, and C(O) with the provisothat (CR³⁷R³⁸)_(b) is bonded to E⁰; R³⁷ and R³⁸ are independentlyselected from the group consisting of hydrido, halo, alkyl, andhaloalkyl.
 7. The compound as recited in claim 6 having the FormulaI-MPS:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of fluoro, chloro, hydroxy, hydroxymethyl,amino, aminomethyl, methoxy, trifluoromethoxy, N-methylamino, methythio,and trifluoromethylthio; B is selected from the group consisting ofphenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl,2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl,3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl,2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl,4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to thecarbon at the point of attachment may be substituted by R³², the othercarbon adjacent to the carbon at the point of attachment may besubstituted by R³⁶, a carbon adjacent to R³² and two atoms from thecarbon at the point of attachment may be substituted by R³³, a carbonadjacent to R³⁶ and two atoms from the carbon at the point of attachmentmay be substituted by R³⁵, and any carbon adjacent to both R³³ and R³⁵may be substituted by R³⁴; R³², R³³, R³⁴, R³⁵, and R³⁶ are independentlyselected from the group consisting of hydrido, amidino, guanidino,dimethylsulfonium, carboxy, methoxy, ethoxy, isopropoxy, propoxy,hydroxy, amino, methoxyamino, ethoxyamino, thio, nitro, aminomethyl,1-aminoethyl, 2-aminoethyl, N-N-methylamino, dimethylamino,N-ethylamino, methylthio, ethylthio, trifluoromethylthio,methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl, propanoyl,trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl,2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, cyano, and Q^(b); B is selected from thegroup consisting of 1-propenyl, propyl, isopropyl, butyl, 2-butenyl,3-butenyl, sec-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl,3-pentenyl, 4-pentenyl, 2-pentyl, 1-methyl-2-butenyl,1-methyl-3-butenyl, 3-pentyl, 1-ethyl-2-propenyl, 2-methylbutyl,2-methyl-2-butenyl, 2-methyl-3-butenyl, 3-methylbutyl,3-methyl-2-butenyl, 3-methyl-3-butenyl, 2,2-difluoropropyl,2-trifluoromethyl-3,3,3-trifluoropropyl, 1,1,1,2,2,2-hexafluoropropyl,3,3,3-trifluoroprop-1-yl, and 3,3,3-trifluoroprop-2-yl, wherein eachmember of group B may be optionally substituted at any carbon up to andincluding 5 atoms from the point of attachment of B to A with one ormore of the group consisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆; B isselected from the group consisting of cyclopropyl, cyclobutyl,oxetan-2-yl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl,thiaetan-2-yl, thiaetan-3-yl, wherein each ring carbon may be optionallysubstituted with R₃₃, a ring carbon and nitrogen atoms adjacent to thecarbon atom at the point of attachment may be optionally substitutedwith R₉ or R₁₃, a ring carbon or nitrogen atom adjacent to the R₉position and two atoms from the point of attachment may be substitutedwith R₁₀, and a ring carbon or nitrogen atom adjacent to the R₁₃position and two atoms from the point of attachment may be substitutedwith R₁₂; R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independently selected from thegroup consisting of amidino, guanidino, dimethylsulfonium, carboxy,methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino,ethoxyamino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-methylamino,dimethylamino, N-ethylamino, methylsulfinyl, ethylsulfinyl,methylsulfonyl, ethylsulfonyl, amidosulfonyl, N-methylamidosulfonyl,N,N-dimethylamidosulfonyl, acetyl, propanoyl, trifluoroacetyl,pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano; A is selected from the groupconsisting of single covalent bond, O, C(O), CH₂, CH₃CH, CF₃CH,CH₃CC(O), CF₃CC(O), CC(O)CCH₃, C(O)CCF₃, CH₂C(O), and (O)CCH₂; R¹ isselected from the group consisting of hydrido, methyl, ethyl, propyl,methoxy, ethoxy, N-methylamino, dimethylamino, N-ethylamino, methylthio,ethylthio, trifluoromethylthio, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo; R² is selectedfrom the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl,3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl,3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl,2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl,4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and1,3,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the pointof attachment may be substituted by R⁹, the other carbon adjacent to thecarbon at the point of attachment may be substituted by R¹³, a carbonadjacent to R⁹ and two atoms from the carbon at the point of attachmentmay be substituted by R¹⁰, a carbon adjacent to R¹³ and two atoms fromthe carbon at the point of attachment may be substituted by R¹², and anycarbon adjacent to both R¹⁰ and R¹² may be substituted by R¹¹; K isCR^(4a)R^(4b) wherein R^(4a) and R^(4b) are independently selected fromthe group consisting of chloro, fluoro, and hydrido; E⁰ is E¹, when K isCR^(4a)R^(4b), wherein E¹ is selected from the group consisting of acovalent single bond, C(O)N(H), (H)NC(O), S(O)₂N(H), N(H)S(O)₂,S(O)₂N(H)C(O), and C(O)N(H)S(O)₂; K is selected from the groupconsisting of N(H) and CH₂N(H); E⁰ is E², when K is selected from thegroup consisting of N(H) and CH₂N(H), wherein E² is selected from thegroup consisting of C(O)N(H), (H)NC(O), S(O)₂N(H), N(H)S(O)₂,S(O)₂N(H)C(O), and C(O)N(H)S(O)₂; Y⁰ is selected from the group offormulas consisting of:

R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, amidino, guanidino, methoxy, ethoxy, isopropoxy,methylthio, ethylthio, trifluoromethylthio, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl,trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo,acetyl, propanoyl, trifluoroacetyl, pentafluoropropanoyl,methoxycarbonyl, ethoxycarbonyl, and cyano; Q^(b) is selected, whenbonded to a carbon, from the group consisting of NR²⁰R²¹, ⁺NR²⁰R²¹R²²,dimethylsulfonium, methylethylsulfonium, diethylsulfonium,trimethylphosphonium, C(NR²⁵)NR²³R²⁴, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with theprovisos that no more than one of R²⁰, R²¹, and R²² is hydroxy, methoxy,ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino, or aminoand that no more than one of R²³, R²⁴, and R²⁶ is hydroxy, methoxy,ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino, or aminowhen two of the group consisting of R²³, R²⁴, and R²⁶ are bonded to thesame atom and that said Q^(b) group is bonded directly to a carbon atom;R²⁰, R²¹, R²², R²³, R²⁴, R²⁵, and R²⁶ are independently selected fromthe group consisting of hydrido, methyl, ethyl, hydroxy, methoxy,ethoxy, 2-aminoethyl, 2-(N-methylamino)ethyl,2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl,N-(2-hydroxyethyl)amino, N,N-bis-(2-hydroxyethyl)amino,N-(2-hydroxyethyl)-N-(2-aminoethyl)amino, N-methylamino,N,N-dimethylamino, and N,N,N-trimethylamino; Q^(b) is selected, whenbonded to a nitrogen, from the group consisting of oxy, methyl, ethyl,2-aminoethyl, 2-(N-methylamino)ethyl, 2-(N,N-dimethylamino)ethyl,2-(N,N,N-trimethylamino)ethyl, N-(2-hydroxyethyl)amino,N,N-bis-(2-hydroxyethyl)amino, amino, hydroxylamino, N-methoxyamino,N-methylamino, N,N-dimethylamino, and N,N,N-trimethylamino; Q^(s) isselected from the group consisting of a single covalent bond, CH₂,CH₃CH, CF₂, CF₃CH, CH₂O, CH₃C(H)O, CF₃C(H)O, CH₂S, CH₃C(H)S, CF₃C(H)S,CH₂C(O), CH₃C(H)C(O), CF₃C(H)C(O), and CF₂C(O) with the proviso thatQ^(s) is bonded to E⁰ through a carbon atom.
 8. The compound as recitedin claim 7 having the Formula I-EMPS:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of fluoro, chloro, hydroxy, hydroxymethyl,amino, aminomethyl, methoxy, trifluoromethoxy, and N-methylamino; B isselected from the group consisting of phenyl, 2-thienyl, 3-thienyl,2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl,3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl,2-pyridyl, 3-pyridyl, and 4-pyridyl, wherein a carbon adjacent to thecarbon at the point of attachment may be substituted by R³², the othercarbon adjacent to the carbon at the point of attachment may besubstituted by R³⁶, a carbon adjacent to R³² and two atoms from thecarbon at the point of attachment may be substituted by R³³, a carbonadjacent to R³⁶ and two atoms from the carbon at the point of attachmentmay be substituted by R³⁵, and any carbon adjacent to both R³³ and R³⁵may be substituted by R³⁴; R³², R³³, R³⁴, R³⁵, and R³⁶ are independentlyselected from the group consisting of hydrido, amidino, guanidino,methoxy, ethoxy, hydroxy, amino, methoxyamino, ethoxyamino, aminomethyl,1-aminoethyl, 2-aminoethyl, N-N-methylamino, dimethylamino,N-ethylamino, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, fluoro, chloro, bromo, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, methoxycarbonyl,ethoxycarbonyl, cyano, and Q^(b); B is selected from the groupconsisting of propyl, isopropyl, butyl, sec-butyl, isobutyl, 1-pentyl,2-pentyl, 3-pentyl, 2-methylbutyl, 3-methylbutyl, 2,2-difluoropropyl,2-trifluoromethyl-3,3,3-trifluoropropyl, 1,1,1,2,2,2-hexafluoropropyl,3,3,3-trifluoroprop-1-yl, and 3,3,3-trifluoroprop-2-yl, wherein eachmember of group B may be optionally substituted at any carbon up to andincluding 5 atoms from the point of attachment of B to A with one ormore of the group consisting of R₃₂, R₃₃, R₃₄, R₃₅, and R₃₆; B isselected from the group consisting of cyclopropyl, cyclobutyl,oxetan-2-yl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl,thiaetan-2-yl, thiaetan-3-yl, wherein each ring carbon may be optionallysubstituted with R₃₃, a ring carbon and nitrogen atoms adjacent to thecarbon atom at the point of attachment may be optionally substitutedwith R₉ or R₁₃, a ring carbon or nitrogen atom adjacent to the R₉position and two atoms from the point of attachment may be substitutedwith R₁₀, and a ring carbon or nitrogen atom adjacent to the R₁₃position and two atoms from the point of attachment may be substitutedwith R₁₂; R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independently selected from thegroup consisting of amidino, guanidino, carboxy, methoxy, ethoxy,hydroxy, amino, methoxyamino, ethoxyamino, aminomethyl, 1-aminoethyl,2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, acetyl,propanoyl, trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, carboxymethyl, methoxycarbonyl,ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano; A is selected from the groupconsisting of single covalent bond, O, C(O), CH₂, CH₂C(O), and (O)CCH₂;R¹ is selected from the group consisting of hydrido, methyl, ethyl,methoxy, ethoxy, N-methylamino, dimethylamino, N-ethylamino,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro,and bromo; R² is selected from the group consisting of phenyl,2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl,2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl,3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl,2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl,4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to thecarbon at the point of attachment may be substituted by R⁹, the othercarbon adjacent to the carbon at the point of attachment may besubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment may be substituted by R¹⁰, a carbonadjacent to R¹³ and two atoms from the carbon at the point of attachmentmay be substituted by R¹², and any carbon adjacent to both R¹⁰ and R¹²may be substituted by R¹¹; K is CR^(4a)R^(4b) wherein R^(4a) and R^(4b)are independently selected from the group consisting of chloro, fluoro,and hydrido; E⁰ is E¹, when K is CR^(4a)R^(4b), wherein E¹ is selectedfrom the group consisting of a covalent single bond, C(O)N(H), (H)NC(O),S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂; K is selectedfrom the group consisting of N(H) and CH₂N(H); E⁰ is E², when K isselected from the group consisting of N(H) and CH₂N(H), wherein E^(Z) isselected from the group consisting of C(O)N(H), (H)NC(O), S(O)₂N(H),N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂; Y⁰ is selected from thegroup of formulas consisting of:

R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from the groupconsisting of hydrido, methoxy, ethoxy, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro,chloro, bromo, acetyl, trifluoroacetyl, methoxycarbonyl, ethoxycarbonyl,and cyano; Q^(b) is selected from the group consisting of NR²⁰R²¹,⁺NR²⁰R²¹R²², dimethylsulfonium, methylethylsulfonium, diethylsulfonium,trimethylphosphonium, C(NR²⁵)NR²³R²⁴, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),C(O)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), N(R²⁶)N(R²⁶)C(NR²⁵)N(R²³)(R²⁴),N(R²⁶)N(R²⁶)SO₂N(R²³)(R²⁴), C(O)NR²³R²⁴, and C(O)NR²³R²⁴ with theprovisos that no more than one of R²⁰, R²¹, and R²² is hydroxy, methoxy,ethoxy, N-methylamino, N,N-dimethylamino, and N,N,N-trimethylamino, oramino and that no more than one of R²³, R²⁴, and R²⁶ is hydroxy,methoxy, ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino,or amino when two of the group consisting of R²³, R²⁴, and R²⁶ arebonded to the same atom and that said Q^(b) group is bonded directly toa carbon atom; R²⁰, R²¹, R²², R²³, R²⁴, R²⁵, and R²⁶ are independentlyselected from the group consisting of hydrido, methyl, ethyl, hydroxy,methoxy, ethoxy, 2-aminoethyl, 2-(N-methylamino)ethyl,2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl,N-(2-hydroxyethyl)amino, N,N-bis-(2-hydroxyethyl)amino,N-(2-hydroxyethyl)-N-(2-aminoethyl)amino, N-methylamino,N,N-dimethylamino, and N,N,N-trimethylamino; Q^(s) is selected from thegroup consisting of a single covalent bond, CH₂, CH₃CH, CF₂, CF₃CH,CH₂O, CH₃C(H)O, CF₃C(H)O, CH₂C(O), CH₃C(H)C(O), CF₃C(H)C(O), and CF₂C(O)with the proviso that Q^(s) is bonded to E⁰ through a carbon atom.
 9. Acomposition for inhibiting thrombotic conditions in blood comprising acompound of any one of claims 1 through 8 and a pharmaceuticallyacceptable carrier.
 10. A method for inhibiting thrombotic conditions inblood comprising adding to blood a therapeutically effective amount of acomposition of claim
 9. 11. A method for inhibiting formation of bloodplatelet aggregates in blood comprising adding to blood atherapeutically effective amount of a composition of claim
 9. 12. Amethod for inhibiting thrombus formation in blood comprising adding toblood a therapeutically effective amount of a composition of claim 9.13. A method for treating or preventing venuous thromboembolism andpulmonary embolism in a mammal comprising administering to the mammal atherapeutically effective amount of a composition of claim
 9. 14. Amethod for treating or preventing deep vein thrombosis in a mammalcomprising administering to the mammal a therapeutically effectiveamount of a composition of claim
 9. 15. A method for treating orpreventing cardiogenic thromboembolism in a mammal comprisingadministering to the mammal a therapeutically effective amount of acomposition of claim
 9. 16. A method for treating or preventingthromboembolic stroke in humans and other mammals comprisingadministering to the mammal a therapeutically effective amount of acomposition of claim
 9. 17. A method for treating or preventingthrombosis associated with cancer and cancer chemotherapy in humans andother mammals comprising administering to the mammal a therapeuticallyeffective amount of a composition of claim
 9. 18. A method for treatingor preventing unstable angina in humans and other mammals comprisingadministering to the mammal a therapeutically effective amount of acomposition of claim
 9. 19. A method for inhibiting thrombus formationin blood comprising adding to blood a therapeutically effective amountof a compound of any one of claims 1 through 8 with a therapeuticallyeffective amount of fibrinogen receptor antagonist.
 20. The use of acompound of any one of claims 1 through 8, or a pharmaceuticallyacceptable salt thereof, in the manufacture of medicament for inhibitingthrombus formation, treating thrombus formation, or preventing thrombusformation in a mammal.
 21. A compound of the Formula:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of halo, haloalkyl, hydroxy, hydroxyalkyl,amino, aminoalkyl, amidino, carboxy, carboxamido, alkylsulfinyl, acyl,cyano, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ is alkyl or haloalkyl; B isphenyl or a heteroaryl of 5 or 6 ring members, wherein a nitrogen with aremovable hydrogen or a carbon adjacent to the carbon at the point ofattachment of said phenyl or heteroaryl ring to A is optionallysubstituted by R³², a nitrogen with a removable hydrogen or a carbon atthe other position adjacent to the point of attachment is optionallysubstituted by R³⁶, a nitrogen with a removable hydrogen or a carbonadjacent to R³² and two atoms from the point of attachment is optionallysubstituted by R³³, a nitrogen with a removable hydrogen or a carbonadjacent to R³⁶ and two atoms from the point of attachment is optionallysubstituted by R³⁵, and a nitrogen with a removable hydrogen or a carbonadjacent to both R³³ and R³⁵ is optionally substituted by R³⁴; R⁹, R¹⁰,R¹¹, R¹², R¹³, R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selectedfrom the group consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkylenedioxy, haloalkylthio, alkanoyloxy, alkoxy,cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy,heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy, alkoxyalkyl,haloalkoxylalkyl, hydroxy, amino, alkoxyamino, nitro, alkylamino,N-alkyl-N-arylamino, arylamino, aralkylamino, heteroarylamino,heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino,alkylthio, alkylthioalkyl, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl,cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfonyl, arylsulfonyl,aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl,alkylsulfonylalkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl,heteroaryl, heterocyclyl, alkylsulfonamido, amidosulfonyl, alkanoyl,haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy,hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl, haloalkoxyalkyl,carboxyalkyl, carboalkoxy, carboxy, carboxamido, carboxamidoalkyl, andcyano; R³², R³³, R³⁴, R³⁵, and R³⁶ are independently optionally Q^(b); Bis optionally selected from the group consisting of hydrido,trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8alkynyl, and C2-C8 haloalkyl, wherein each member of group B isoptionally substituted at any carbon up to and including 6 atoms fromthe point of attachment of B to A with one or more of the groupconsisting of R³², R³³, R³⁴, R³⁵, and R³⁶; B is optionally a C3-C12cycloalkyl or C4-C9 saturated heterocyclyl, wherein each ring carbon isoptionally substituted with R³³, a ring carbon other than the ringcarbon at the point of attachment of B to A is optionally substitutedwith oxo provided that no more than one ring carbon is substituted byoxo at the same time, ring carbons and a nitrogen adjacent to the carbonatom at the point of attachment are optionally substituted with R⁹ orR¹³, a ring carbon or nitrogen atom adjacent to the R⁹ position and twoatoms from the point of attachment is optionally substituted with R¹⁰, aring carbon or nitrogen adjacent to the R¹³ position and two atoms fromthe point of attachment is optionally substituted with R¹², a ringcarbon or nitrogen three atoms from the point of attachment and adjacentto the R¹⁰ position is optionally substituted with R¹¹, a ring carbon ornitrogen three atoms from the point of attachment and adjacent to theR¹² position is optionally substituted with R³³, and a ring carbon ornitrogen four atoms from the point of attachment and adjacent to the R¹¹and R³³ positions is optionally substituted with R³⁴; A is selected fromthe group consisting of a bond, (W⁷)_(rr)—(CH(R¹⁵))_(pa), and(CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is 0 or 1, pa is an integer selectedfrom 0 through 6, and W⁷ is selected from the group consisting of O, S,C(O), (R⁷)NC(O), (R⁷)NC(S), and N(R⁷) with the proviso that no more thanone of the group consisting of rr and pa is 0 at the same time and withthe further proviso that W⁷ is selected from other than C(O) when W⁷ isbonded to Ψ; R⁷ is selected from the group consisting of hydrido,hydroxy, and alkyl; R¹⁵ is selected from the group consisting ofhydrido, hydroxy, halo, alkyl, and haloalkyl; Ψ is NH or NOH; X⁰ and R¹are independently selected from the group consisting of hydrido, alkyl,alkenyl, cyano, halo, haloalkyl, haloalkoxy, haloalkylthio, amino,aminoalkyl, alkylamino, amidino, hydroxy, hydroxyamino, alkoxy,hydroxyalkyl, alkoxyamino, thiol, and alkylthio; R² is Z⁰-Q; Z⁰ isselected from the group consisting of a bond, (CR⁴¹R⁴²)_(q) wherein q isan integer selected from 1 through 3, and (CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p)wherein g and p are integers independently selected from 0 through 3 andW⁰ is selected from the group consisting of O, S, C(O), S(O), N(R⁴¹),and ON(R⁴¹); Z⁰ is optionally (CH(R⁴¹))_(e)—W²²—(CH(R⁴²))_(h) wherein eand h are independently 0 or 1 and W²² is selected from the groupconsisting of CR⁴¹═CR⁴², 1,2-cyclopropyl, 1,2-cyclobutyl,1,2-cyclohexyl, 1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl,2,3-morpholinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl,3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 2,3-piperazinyl,2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl,2,4-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 1,2-pyrrolidinyl,1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl,3,4-pyrrolidinyl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl,2,5-tetrahydrofuranyl, and 3,4-tetrahydrofuranyl, wherein Z⁰ is directlybonded to the benzene ring and W²² is optionally substituted with one ormore substituents selected from the group consisting of R⁹, R¹⁰, R¹¹,R¹², and R¹³; R⁴¹ and R⁴² are independently selected from the groupconsisting of amidino, hydroxyamino, hydrido, hydroxy, amino, and alkyl;Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a nitrogenwith a removable hydrogen or a carbon adjacent to the carbon at thepoint of attachment of said phenyl or heteroaryl ring to Z⁰ isoptionally substituted by R⁹, a nitrogen with a removable hydrogen or acarbon at the other position adjacent to the point of attachment isoptionally substituted by R¹³, a nitrogen with a removable hydrogen or acarbon adjacent to R⁹ and two atoms from the point of attachment isoptionally substituted by R¹⁰, a nitrogen with a removable hydrogen or acarbon adjacent to R¹³ and two atoms from the point of attachment isoptionally substituted by R¹², and a nitrogen with a removable hydrogenor a carbon adjacent to both R¹⁰ and R¹² is optionally substituted byR¹¹; Q is optionally hydrido with the proviso that Z⁰ is selected fromother than a bond; K is CR^(4a)R^(4b); R^(4a) and R^(4b) areindependently selected from the group consisting of halo, hydrido,hydroxy, alkyl, and haloalkyl; with the proviso that K is CR^(4a)R^(4b),is E¹ wherein E¹ is selected from the group consisting of a covalentsingle bond, C(O)N(H), (H)NC(O), C(S)N(H), (H)NC(S), S(O)₂N(H),N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂; K is optionally(CH(R¹⁴))_(j)-T wherein j is 0 or 1 and T is a bond or N(R⁷) with theproviso that (CH(R¹⁴))_(j) is bonded to the phenyl ring; R¹⁴ is selectedfrom the group consisting of hydrido, halo, alkyl, and haloalkyl; E⁰,with the proviso that K is (CH(R¹⁴))_(j)-T, is E² wherein E² is selectedfrom the group consisting of C(O)N(H), (H)NC(O), C(S)N(H), (H)NC(S),S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), and C(O)N(H)S(O)₂; Y⁰ is phenyl ora heteroaryl of 5 or 6 ring members, wherein one carbon of said phenylor said heteroaryl is substituted by Q^(s), a carbon two or threecontiguous atoms from the point of attachment of Q^(s) to said phenyl orsaid heteroaryl to said phenyl or said heteroaryl is substituted byQ^(b), a carbon adjacent to the point of attachment of Q^(s) isoptionally substituted by R¹⁷, another carbon adjacent to the point ofattachment of Q^(s) is optionally substituted by R¹⁸, a carbon adjacentto Q^(b) is optionally substituted by R¹⁶, and another carbon adjacentto Q^(b) bis optionally substituted by R¹⁹; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, nitro,alkoxyamino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl,alkanoyl, haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkoxy,hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboalkoxy, and cyano; R¹⁶or R¹⁹ is optionally selected from the group consisting of NR²⁰R²¹,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the proviso that R¹⁶,R¹⁹, and Q^(b) are not simultaneously hydrido; Q^(b) is selected fromthe group consisting of NR²⁰R²¹, aminoalkyl, hydrido,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the proviso that nomore than one of R²⁰ and R²¹ is selected from the group consisting ofhydroxy, amino, alkylamino, and dialkylamino at the same time, with thefurther proviso that no more than one of R²³ and R²⁴ is selected fromthe group consisting of hydroxy, amino, alkylamino, and dialkylamino atthe same time; R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ are independentlyselected from the group consisting of hydrido, alkyl, hydroxy,aminoalkyl, amino, dialkylamino, alkylamino, and hydroxyalkyl; Q^(s) isselected from the group consisting of a bond, (CR³⁷R³⁸)_(b) wherein b isan integer selected from 1 through 4, and (CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d)wherein c and d are integers independently selected from 1 through 3 andW¹ is selected from the group consisting of C(O)N(R¹⁴), (R¹⁴)NC(O),S(O), S(O)₂, S(O)₂N(R¹⁴), N(R¹⁴)S(O)₂, and N(R¹⁴), with the proviso thatR¹⁴ is selected from other than halo when directly bonded to N, and withthe additional proviso that (CR³⁷R³⁸)_(b) and (CH(R¹⁴))_(c) are bondedto E⁰; R³⁷ and R³⁸ are independently selected from the group consistingof hydrido, alkyl, and haloalkyl; R³⁸ is optionally aroyl orheteroaroyl, wherein R³⁸ is optionally substituted with one or moresubstituents selected from the group consisting of R¹⁶, R¹⁷, R¹⁸, andR¹⁹; Y⁰ is optionally Y^(AT) wherein Y^(AT) is Q^(b)-Q^(s); Y⁰ isoptionally Q^(b)-Q^(ss) wherein Q^(ss) is(CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h), wherein e and h are independently 1 or 2and W² is CR^(4a)═CR^(4b), with the proviso that (CH(R¹⁴))_(e) is bondedto E⁰.
 22. Compound of claim 21 of the Formula:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of halo, haloalkyl, hydroxy, hydroxyalkyl,amino, aminoalkyl, amidino, carboxy, carboxamido, alkylsulfinyl, formyl,cyano, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ is alkyl or haloalkyl; B isphenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacentto the carbon at the point of attachment of said phenyl or heteroarylring to A is optionally substituted by R³², the other carbon adjacent tothe carbon at the point of attachment is optionally substituted by R³⁶,a carbon adjacent to R³² and two atoms from the carbon at the point ofattachment is optionally substituted by R³³, a carbon adjacent to R³⁶and two atoms from the carbon at the point of attachment is optionallysubstituted by R³⁵, and any carbon adjacent to both R³³ and R³⁵ isoptionally substituted by R³⁴; R³², R³³, R³⁴, R³⁵, and R³⁶ areindependently selected from the group consisting of hydrido, acetamido,haloacetamido, amidino, guanidino, alkylenedioxy, haloalkylthio,alkanoyloxy, alkoxy, hydroxy, amino, alkoxyamino, haloalkanoyl, nitro,alkylamino, alkylthio, aryl, aralkyl, cycloalkyl, cycloalkylalkyl,heteroaryl, heterocyclyl, alkylsulfonamido, amidosulfonyl, alkyl,alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyalkyl,hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxamido, cyano,and Q^(b); B is optionally selected from the group consisting ofhydrido, trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl,C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B isoptionally substituted at any carbon up to and including 6 atoms fromthe point of attachment of B to A with one or more of the groupconsisting of R³², R³³, R³⁴, R³⁵, and R³⁶; B is optionally a C3-C12cycloalkyl or a C4-C9 saturated heterocyclyl, wherein each ring carbonis optionally substituted with R³³, a ring carbon other than the ringcarbon at the point of attachment of B to A is optionally substitutedwith oxo provided that no more than one ring carbon is substituted byoxo at the same time, ring carbons and a nitrogen adjacent to the carbonatom at the point of attachment are optionally substituted with R⁹ orR¹³, a ring carbon or nitrogen atom adjacent to the R⁹ position and twoatoms from the point of attachment is optionally substituted with R¹⁰, aring carbon or nitrogen atom adjacent to the R¹³ position and two atomsfrom the point of attachment is optionally substituted with R¹², a ringcarbon or nitrogen atom three atoms from the point of attachment andadjacent to the R¹⁰ position is optionally substituted with R¹¹, a ringcarbon or nitrogen atom three atoms from the point of attachment andadjacent to the R¹² position is optionally substituted with R³³, and aring carbon or nitrogen atom four atoms from the point of attachment andadjacent to the R¹¹ and R³³ positions is optionally substituted withR³⁴; R⁹, R¹⁰, R¹¹, R¹², and R¹³ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, alkoxyamino,alkanoyl, haloalkanoyl, amidino, guanidino, alkylenedioxy,haloalkylthio, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy,heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy,hydroxy, amino, alkylamino, N-alkyl-N-arylamino, arylamino,aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino,heterocyclylalkylamino, alkylthio, alkylsulfinyl, arylsulfinyl,aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfamido,alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl,heteroarylsulfonyl, amidosulfonyl, alkyl, aryl, aralkyl, cycloalkyl,cycloalkylalkyl, heteroaryl, heterocyclyl, halo, haloalkyl, haloalkoxy,hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy,carboxyalkyl, carboxamido, and cyano; A is bond or(CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is 0 or 1, pa is an integer selectedfrom 0 through 3, and W⁷ is selected from the group consisting of O, S,C(O), (R⁷)NC(O), (R⁷)NC(S), and N(R⁷), with the further proviso that W⁷is selected from other than C(O) when W⁷ is bonded to the N(H) on thebenzene ring; R⁷ is selected from the group consisting of hydrido,hydroxy and alkyl; R¹⁵ is selected from the group consisting of hydrido,hydroxy, halo, alkyl, and haloalkyl; R¹ and X⁰ are independentlyselected from the group consisting of hydrido, alkyl, cyano, halo,haloalkyl, haloalkoxy, amino, aminoalkyl, alkylamino, amidino, hydroxy,hydroxyamino, alkoxy, hydroxyalkyl, alkoxyamino, thiol, and alkylthio;R² is Z⁰-Q; Z⁰ is selected from the group consisting of a bond,(CR⁴¹R⁴²)_(q) wherein q is 1 or 2, and (CH(R⁴¹))_(g)—W⁰—(CH(R⁴²))_(p)wherein g and p are integers independently selected from 0 through 3 andW⁰ is selected from the group consisting of O, S, C(O), S(O), N(R⁴¹),and ON(R⁴¹); Z⁰ is optionally (CH(R⁴¹))_(e)—W²²—(CH(R⁴²))_(h) wherein eand h are independently 0 or 1 and W²² is selected from the groupconsisting of CR⁴¹═CR⁴², 1,2-cyclopropyl, 1,2-cyclobutyl,1,2-cyclohexyl, 1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl,2,3-morpholinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl,3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 2,3-piperazinyl,2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl,2,4-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 1,2-pyrrolidinyl,1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl,3,4-pyrrolidinyl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl,2,5-tetrahydrofuranyl, and 3,4-tetrahydrofuranyl, wherein Z⁰ is directlybonded to the benzene ring and W²² is optionally substituted with one ormore substituents selected from the group consisting of R⁹, R¹⁰, R¹¹,R¹², and R¹³; R⁴¹ and R⁴² are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, and amino; Q is phenyl or aheteroaryl of 5 or 6 ring members, wherein a carbon adjacent to thecarbon at the point of attachment of said phenyl or heteroaryl ring toZ⁰ is optionally substituted by R⁹, the other carbon adjacent to thecarbon at the point of attachment is optionally substituted by R¹³, acarbon adjacent to R⁹ and two atoms from the carbon at the point ofattachment is optionally substituted by R¹⁰, a carbon adjacent to R¹³and two atoms from the carbon at the point of attachment is optionallysubstituted by R¹², and any carbon adjacent to both R¹⁰ and R¹² isoptionally substituted by R¹¹; Q is optionally hydrido with the provisothat Z⁰ is other than a bond; K is CR^(4a)R^(4b); R^(4a) and R^(4b) areindependently selected from the group consisting of halo, hydrido, andhydroxy; E⁰, with the proviso that K is CR^(4a)R^(4b), is E¹ wherein E¹is selected from the group consisting of a covalent single bond,C(O)N(H), (H)NC(O), S(O)₂N(H), and N(H)S(O)₂; K is optionally(CH(R¹⁴))_(j)-T wherein j is 0 or 1 and T is a bond or N(R⁷) with theproviso that (CH(R¹⁴))_(j) is bonded to the phenyl ring; R¹⁴ is hydridoor halo; E⁰, with the proviso that K is (CH(R¹⁴))_(j)-T, is E² whereinE² is selected from the group consisting of C(O)N(H), (H)NC(O),C(S)N(H), (H)NC(S), S(O)₂N(H), N(H)S(O)₂, S(O)₂N(H)C(O), andC(O)N(H)S(O)₂; Y⁰ is phenyl or a heteroaryl of 5 or 6 ring members,wherein one carbon of said phenyl or said heteroaryl is substituted byQ^(s), a carbon two or three atoms from the point of attachment of Q^(s)to said phenyl or said heteroaryl is substituted by Q^(b), a carbonadjacent to the point of attachment of Q^(s) is optionally substitutedby R¹⁷, another carbon adjacent to the point of attachment of Q^(s) isoptionally substituted by R¹⁸, a carbon adjacent to Q^(b) is optionallysubstituted by R¹⁶, and another carbon adjacent to Q^(b) is optionallysubstituted by R¹⁹; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selectedfrom the group consisting of hydrido, amidino, guanidino, carboxy,haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, alkylamino,alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl,halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano; R¹⁶ orR¹⁹ is optionally selected from the group consisting of NR²⁰R²¹,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the proviso that R¹⁶,R¹⁹, and Q^(b) are not simultaneously hydrido; Q^(b) is selected fromthe group consisting of NR²⁰R²¹, hydrido, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), andC(NR²⁵)NR²³R²⁴, with the proviso that no more than one of R²⁰ and R²¹ isselected from the group consisting of hydroxy, amino, alkylamino, anddialkylamino at the same time, with the further proviso that no morethan one of R²³ and R²⁴ is selected from the group consisting ofhydroxy, amino, alkylamino, and dialkylamino at the same time; R²⁰, R²¹,R²³, R²⁴, R²⁵, and R²⁶ are independently selected from the groupconsisting of hydrido, alkyl, hydroxy, amino, alkylamino anddialkylamino; Q^(s) is selected from the group consisting of a bond,(CR³⁷R³⁸)_(b) wherein b is an integer selected from 1 through 4, and(CH(R¹⁴))_(c)—W¹—(CH(R¹⁵))_(d) wherein c and d are integersindependently selected from 1 through 3 and W¹ is selected from thegroup consisting of C(O)N(R¹⁴), (R¹⁴)NC(O), S(O), S(O)₂, S(O)₂N(R¹⁴),N(R¹⁴)S(O)₂, and N(R¹⁴), with the proviso that R¹⁴ is selected fromother than halo when directly bonded to N, and with the additionalproviso that (CR³⁷R³⁸)_(b) and (CR³⁷R³⁸)_(b), and (CH(R¹⁴))_(c) arebonded to E⁰; R³⁷ and R³⁸ are independently selected from the groupconsisting of hydrido, alkyl, and haloalkyl; R³⁸ is optionally aroyl orheteroaroyl, wherein R³⁸ is optionally substituted with one or moresubstituents selected from the group consisting of R¹⁶, R¹⁷, R¹⁸, andR¹⁹; Y⁰ is optionally Y^(AT) wherein Y^(AT) is Q^(b)-Q^(s); Y⁰ isoptionally Q^(b)-Q^(ss) wherein Q^(ss) is(CH(R¹⁴))_(e)—W²—(CH(R¹⁵))_(h), wherein e and h are independently 1 or 2and W² is CR^(4a)═CR^(4b) with the proviso that (CH(R¹⁴))_(e) is bondedto E⁰.
 23. Compound of claim 22 or a pharmaceutically acceptable saltthereof, wherein;

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of halo, haloalkyl, hydroxy, hydroxyalkyl,amino, aminoalkyl, cyano, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ is alkyl orhaloalkyl; B is phenyl or a heteroaryl of 5 or 6 ring members, wherein acarbon adjacent to the carbon at the point of attachment of said phenylor heteroaryl ring to A is optionally substituted by R³², the othercarbon adjacent to the carbon at the point of attachment is optionallysubstituted by R³⁶, a carbon adjacent to R³² and two atoms from thecarbon at the point of attachment is optionally substituted by R³³, acarbon adjacent to R³⁶ and two atoms from the carbon at the point ofattachment is optionally substituted by R³⁵, and any carbon adjacent toboth R³³ and R³⁵ is optionally substituted by R³⁴; R³², R³³, R³⁴, R³⁵,and R³⁶ are independently selected from the group consisting of hydrido,acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino,alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo,haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy,carboxy, carboxamido, cyano, and Q^(b); A is a bond or(CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is 0 or 1, pa is an integer selectedfrom 0 through 3, and W⁷ is (R⁷)NC(O) or N(R⁷); R⁷ is selected from thegroup consisting of hydrido, hydroxy and alkyl; R¹⁵ is selected from thegroup consisting of hydrido, halo, alkyl, and haloalkyl; R¹ and X^(o)are independently selected from the group consisting of hydrido,hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl, alkoxy,alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, haloalkyl,haloalkoxy, and halo; R² is Z⁰-Q; Z⁰ is selected from the groupconsisting of a bond, CH₂, CH₂CH₂, W⁰—(CH(R⁴²))_(p) wherein p is 0 or 1and W⁰ is selected from the group consisting of O, S, and N(R⁴¹); R⁴¹and R⁴² are independently hydrido or alkyl; Q is phenyl or a heteroarylof 5 or 6 ring members, wherein a carbon adjacent to the carbon at thepoint of attachment of said phenyl or heteroaryl ring to Z⁰ isoptionally substituted by R⁹, the other carbon adjacent to the carbon atthe point of attachment is optionally substituted by R¹³, a carbonadjacent to R⁹ and two atoms from the carbon at the point of attachmentis optionally substituted by R¹⁰, a carbon adjacent to R¹³ and two atomsfrom the carbon at the point of attachment is optionally substituted byR¹², and any carbon adjacent to both R¹⁰ and R¹² is optionallysubstituted by R¹¹; R⁹, R¹¹, and R¹³ are independently selected from thegroup consisting of hydrido, hydroxy, amino, amidino, guanidino,alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl,amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl,hydroxyhaloalkyl, carboxy, carboxamido, and cyano; R¹⁰ and R¹² areindependently selected from the group consisting of hydrido, acetamido,haloacetamido, amidino, guanidino, alkyl, aryl, aralkyl, cycloalkyl,cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy,cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy,heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino,alkylamino, arylamino, aralkylamino, heteroarylamino,heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino,alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl,cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl,cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl,aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo,haloalkyl, and cyano; Y⁰ is phenyl or a heteroaryl of 5 or 6 ringmembers, wherein one carbon of said phenyl or said heteroaryl issubstituted by Q^(s), a carbon two or three atoms from the point ofattachment of Q^(s) to said phenyl or said heteroaryl is substituted byQ^(b), a carbon adjacent to the point of attachment of Q^(s) isoptionally substituted by R¹⁷, another carbon adjacent to the point ofattachment of Q^(s) is optionally substituted by R¹⁸, a carbon adjacentto Q^(b) is optionally substituted by R¹⁶, and another carbon adjacentto Q^(b) is optionally substituted by R¹⁹; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino,alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl,halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano; R¹⁶ orR¹⁹ is optionally NR²⁰R²¹ or C(NR²⁵)NR²³R²⁴, with the proviso that R¹⁶,R¹⁹, and Q^(b) are not simultaneously hydrido; Q^(b) is selected fromthe group consisting of NR²⁰R²¹, hydrido, and C(NR²⁵)NR²³R²⁴, with theproviso that no more than one of R²⁰ and R²¹ is hydroxy at the same timeand with the further proviso that no more than one of R²³ and R²⁴ ishydroxy at the same time; R²⁰, R²¹, R²³, R²⁴, and R²⁵ are independentlyselected from the group consisting of hydrido, alkyl, and hydroxy; Q^(s)is selected from the group consisting of a bond, CH₂, and CH₂CH₂. 24.Compound of claim 23 or a pharmaceutically acceptable salt thereof,wherein; J is selected from the group consisting of fluoro, chloro,trifluoromethyl, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,1,2-dihydroxyethyl, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl,methoxy, trifluoromethoxy, N-methylamino, methythio, andtrifluoromethylthio; B is selected from the group consisting of phenyl,2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl,2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl,3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl,2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl,4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to thecarbon at the point of attachment of said phenyl or heteroaryl ring to Ais optionally substituted by R³², the other carbon adjacent to thecarbon at the point of attachment is optionally substituted by R³⁶, acarbon adjacent to R³² and two atoms from the carbon at the point ofattachment is optionally substituted by R³³, a carbon adjacent to R³⁶and two atoms from the carbon at the point of attachment is optionallysubstituted by R³⁵, and any carbon adjacent to both R³³ and R³⁵ isoptionally substituted by R³⁴; R³², R³³, R³⁴, R³⁵, and R³⁶ areindependently selected from the group consisting of hydrido, amidino,guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy,amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido,N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio,isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, cyano, and Q^(b); A is selected from thegroup consisting of a bond, NH, N(CH₃), N(OH), CH₂, CH₃CH, CF₃CH,NHC(O), N(CH₃)C(O), C(O)NH, C(O)N(CH₃), CH₂CH₂, CH₂CH₂CH₂, CH₃CHCH₂, andCF₃CHCH₂; R¹ and X^(o) are independently selected from the groupconsisting of hydrido, hydroxy, amino, amidino, hydroxyamino,aminomethyl, 1-aminoethyl, methylamino, dimethylamino, cyano, methyl,ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methoxyamino, methylthio,ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro,and bromo; R² is Z⁰-Q; Z⁰ is selected from the group consisting of abond, CH₂, CH₂CH₂, O, S, NH, N(CH₃), OCH₂, SCH₂, N(H)CH₂, and N(CH₃)CH₂;Q is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl,2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl,3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl,2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl,4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and1,3,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the pointof attachment of said phenyl or heteroaryl ring to Z⁰ is optionallysubstituted by R⁹, the other carbon adjacent to the carbon at the pointof attachment is optionally substituted by R¹³, a carbon adjacent to R⁹and two atoms from the carbon at the point of attachment is optionallysubstituted by R¹⁰, a carbon adjacent to R¹³ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹², andany carbon adjacent to both R¹⁰ and R¹² is optionally substituted byR¹¹; R⁹, R¹¹, and R¹³ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl,propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio,isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano; R¹⁰ and R¹² are independentlyselected from the group consisting of hydrido, amidino, guanidino,carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy,ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino,acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl,N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl,N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,N-(3-fluorobenzyl)amidocarbonyl,N-(2-trifluoromethylbenzyl)amidocarbonyl,N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl,N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl,N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy,cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy,cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy,3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino,5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl,4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino,4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy,4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl,5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy,2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy,3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy,2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy,3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy,3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy,4-fluorobenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy,3-fluoro-5-trifluoromethylbenzyloxy,4-fluoro-2-trifluoromethylbenzyloxy,4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy,2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy,4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy,4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy,4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy,4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino,1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino,phenylsulfonyl, 3-trifluoromethoxybenzyloxy,4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy,4-trifluoromethoxyphenoxy, 3-trifluoromethylbenzyloxy,4-trifluoromethylbenzyloxy, 2,4-bis-trifluoromethylbenzyloxy,3-trifluoromethylbenzyl, 3,5-bis-trifluoromethylbenzyloxy,4-trifluoromethylphenoxy, 3-trifluoromethylphenoxy,3-trifluoromethylthiobenzyloxy, 4-trifluoromethylthiobenzyloxy,2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy,3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and3-trifluoromethylthiophenoxy; Y⁰ is selected from the group consistingof: 1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine, 2-Q^(b)-5-Q^(s)-3-R¹⁶-6-R¹⁸pyrazine, 3-Q^(b)-6-Q^(s)-2-R¹⁸-5-R¹⁸-4-R¹⁹ pyidazine,2-Q^(b)-5-Q^(s)-4-R¹⁷-6-R¹⁸ pyrimidine, 5-Q^(b)-2-Q^(s)-4-R¹⁶-6-R¹⁹pyrimidine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹ thiophene,2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹furan, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ furan, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹pyrrole, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ pyrrole, 4-Q^(b)-2-Q^(s)-5-R¹⁹imidazole, 2-Q^(b)-4-Q^(s)-5-R¹⁷ imidazole, 3-Q^(b)-5-Q^(s)-4-R¹⁶isoxazole, 5-Q^(b)-3-Q^(s)-4-R¹⁶ isoxazole, 2-Q^(b)-5-Q^(s)-4-R¹⁶pyrazole, 4-Q^(b)-2-Q^(s)-5-R¹⁹ thiazole, and 2-Q^(b)-5-Q^(s)-4-R¹⁷thiazole; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from thegroup consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy,amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy,amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,dimethylamino, N-ethylamino, methyl thio, ethyl thio, isopropylthio,trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl,ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, and cyano; R¹⁶ or R¹⁹ is optionallyC(NR²⁵)NR²³R²⁴ with the proviso that R¹⁶, R¹⁹, and Q^(b) are notsimultaneously hydrido; Q^(b) is C(NR²⁵)NR²³R²⁴ or hydrido, with theproviso that no more than one of R²³ and R²⁴ is hydroxy at the sametime; R²³, R²⁴, and R²⁵ are independently selected from the groupconsisting of hydrido, methyl, ethyl, and hydroxy; Q^(s) is selectedfrom the group consisting of a bond, CH₂ and CH₂CH₂.
 25. Compound ofclaim 24 or a pharmaceutically acceptable salt thereof, wherein; J isselected from the group consisting of fluoro, chloro, trifluoromethyl,hydroxy, hydroxymethyl, amino, aminomethyl, methoxy, trifluoromethoxy,and N-methylamino; B is selected from the group consisting of2-aminophenyl, 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl,3-carboxyphenyl, 3-carboxy-5-hydroxyphenyl, 3-chlorophenyl,4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl,3,4-difluorophenyl, 3-hydroxyphenyl, 4-hydroxyphenyl,3-methoxyaminophenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl,4-methylphenyl, phenyl, 3-trifluoromethylphenyl, 2-imidazoyl, 2-pyridyl,3-pyridyl, 5-chloro-3-trifluoromethyl-2-pyridyl, 4-pyridyl, 2-thienyl,3-thienyl, and 3-trifluoromethyl-2-pyridyl; A is selected from the groupconsisting of CH₂, CH₃CH, CF₃CH, NHC(O), CH₂CH₂, and CH₂CH₂CH₂; R¹ andX^(o) are independently selected from the group consisting of hydrido,hydroxy, amino, amidino, hydroxyamino, aminomethyl, methylamino, cyano,methyl, trifluoromethyl methoxy, hydroxymethyl, methoxyamino,methylthio, trifluoromethoxy, fluoro, and chloro; R² is Z⁰-Q; Z⁰ isselected from the group consisting of a bond, CH₂, O, S, NH, N(CH₃),OCH₂, and SCH₂; Q is selected from the group consisting of3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl,3-amino-5-benzylphenyl, 3-amino-5-(2-phenylethyl)phenyl,3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenylethylamino)phenyl,3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-benzylamidosulfonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,3-amino-5-(N-ethylamidocarbonyl)phenyl,3-amino-5-(N-isopropylamidocarbonyl)phenyl,3-amino-5-(N-propylamidocarbonyl)phenyl,3-amino-5-(N-isobutylamidocarbonyl)phenyl,3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,3-aminophenyl, 3-amino-5-(4-trifluoromethylbenzylamino)phenyl,3-amino-5-trifluoromethylbenzyloxy)phenyl, 3-carboxyphenyl,3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl,2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,2-fluorophenyl, 3-fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl,3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl,phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; Y⁰ isselected from the group consisting of:1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹thiophene, and 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene; R¹⁶ and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl,fluoro, chloro, and cyano; R¹⁶ or R¹⁹ is optionally C(NR²⁵)NR²³R²⁴ withthe proviso that R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido; R¹⁷and R¹⁸ are independently selected from the group consisting of hydrido,fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano; Q^(b)is C(NR²⁵)NR²³R²⁴ or hydrido; R²³, R²⁴, and R²⁵ are independentlyhydrido or methyl; Q^(s) is CH₂.
 26. Compound of claim 23 of theFormula:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of halo, haloalkyl, hydroxy, hydroxyalkyl,amino, and aminoalkyl; B is phenyl or a heteroaryl of 5 or 6 ringmembers, wherein a carbon adjacent to the carbon at the point ofattachment of said phenyl or heteroaryl ring to A is optionallysubstituted by R³², the other carbon adjacent to the carbon at the pointof attachment is optionally substituted by R³⁶, a carbon adjacent to R³²and two atoms from the carbon at the point of attachment is optionallysubstituted by R³³, a carbon adjacent to R³⁶ and two atoms from thecarbon at the point of attachment is optionally substituted by R³⁵, andany carbon adjacent to both R³³ and R³⁵ is optionally substituted byR³⁴; R³², R³³, R³⁴, R³⁵, and R³⁶ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio,amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl,carboalkoxy, carboxy, carboxamido, cyano, and Q^(b); A is a bond or(CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is 0 or 1, pa is an integer selectedfrom 0 through 3, and W⁷ is N(R⁷); R⁷ is hydrido or alkyl; R¹⁵ isselected from the group consisting of hydrido, halo, alkyl, andhaloalkyl; R¹ and X^(o) are independently selected from the groupconsisting of hydrido, hydroxy, hydroxyamino, amidino, amino, cyano,hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio,alkoxyamino, haloalkyl, haloalkoxy, and halo; R² is Z⁰-Q; Z⁰ is a bond;Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbonadjacent to the carbon at the point of attachment of said phenyl orheteroaryl ring to Z⁰ is optionally substituted by R⁹, the other carbonadjacent to the carbon at the point of attachment is optionallysubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹⁰, acarbon adjacent to R¹³ and two atoms from the carbon at the point ofattachment is optionally substituted by R¹², and any carbon adjacent toboth R¹⁰ and R¹² is optionally substituted by R¹¹; R⁹, R¹¹, and R¹³ areindependently selected from the group consisting of hydrido, hydroxy,amino, amidino, guanidino, alkylamino, alkylthio, alkoxy, alkylsulfinyl,alkylsulfonyl, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy,hydroxyalkyl, carboxy, carboxamido, and cyano; R¹⁰ and R¹² areindependently selected from the group consisting of hydrido, acetamido,haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, hydroxy,amino, alkylamino, alkylsulfonamido, amidosulfonyl, hydroxyalkyl,aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxamido,carboxyalkyl, and cyano; Y⁰ is phenyl or a heteroaryl of 5 or 6 ringmembers, wherein one carbon of said phenyl or said heteroaryl issubstituted by Q^(s), a carbon two or three atoms from the point ofattachment of Q^(s) to said phenyl or said heteroaryl is substituted byQ^(b), a carbon adjacent to the point of attachment of Q^(s) isoptionally substituted by R¹⁷, another carbon adjacent to the point ofattachment of Q^(s) is optionally substituted by R¹⁸, a carbon adjacentto Q^(b) is optionally substituted by R¹⁶, and another carbon adjacentto Q^(b) is optionally substituted by R¹⁹; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino,alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl,halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano; R¹⁶ orR¹⁹ is optionally NR²⁰R²¹ or C(NR²⁵)NR²³R²⁴, with the proviso that R¹⁶,R¹⁹, and Q^(b) are not simultaneously hydrido; Q^(b) is selected fromthe group consisting of NR²⁰R²¹, hydrido, and C(NR²⁵)NR²³R²⁴; R²⁰, R²¹,R²³, R²⁴, and R²⁵ are independently hydrido or alkyl; Q^(s) is CH₂. 27.Compound of claim 26 or a pharmaceutically acceptable salt thereof,wherein; J is selected from the group consisting of fluoro, chloro,trifluoromethyl, hydroxy, hydroxymethyl, amino, and aminomethyl; B isselected from the group consisting of phenyl, 2-thienyl, 3-thienyl,2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl,3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, and 5-isoxazolyl,wherein a carbon adjacent to the carbon at the point of attachment ofsaid phenyl or heteroaryl ring to A is optionally substituted by R³²,the other carbon adjacent to the carbon at the point of attachment isoptionally substituted by R³⁶, a carbon adjacent to R³² and two atomsfrom the carbon at the point of attachment is optionally substituted byR³³, a carbon adjacent to R³⁶ and two atoms from the carbon at the pointof attachment is optionally substituted by R³⁵, and any carbon adjacentto both R³³ and R³⁵ is optionally substituted by R³⁴; R³², R³³, R³⁴,R³⁵, and R³⁶ are independently selected from the group consisting ofhydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy,amino, N-methylamino, dimethylamino, methoxyamino, methylthio,ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl,hydroxymethyl, amidocarbonyl, carboxy, cyano, and Q^(b); A is selectedfrom the group consisting of a bond, NH, N(CH₃), CH₂, CH₃CH, and CH₂CH₂;X^(o) is selected from the group consisting of hydrido, hydroxy, amino,amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl,chloro, and fluoro; R¹ is selected from the group consisting of hydrido,hydroxy, hydroxymethyl, amino, aminomethyl, methylamino, cyano, methyl,trifluoromethyl, methoxy, methylthio, trifluoromethoxy, fluoro, andchloro; R² is selected from the group consisting of phenyl, 2-thienyl,2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl,and 3-pyridyl, wherein a carbon adjacent to the carbon at the point ofattachment of said phenyl or heteroaryl ring to the benzene ring isoptionally substituted by R⁹, the other carbon adjacent to the carbon atthe point of attachment is optionally substituted by R¹³, a carbonadjacent to R⁹ and two atoms from the carbon at the point of attachmentis optionally substituted by R¹⁰, a carbon adjacent to R¹³ and two atomsfrom the carbon at the point of attachment is optionally substituted byR¹², and any carbon adjacent to both R¹⁰ and R¹² is optionallysubstituted by R¹¹; R⁹, R¹¹, and R¹³ are independently selected from thegroup consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy,amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl,carboxy, and cyano; R¹⁰ and R¹² are independently selected from thegroup consisting of hydrido, amidino, amidocarbonyl,N-methylamidocarbonyl, N-benzylamidocarbonyl,N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl,N-(2-trifluoromethylbenzyl)amidocarbonyl,N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl,N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl,N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy,hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy,carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino,dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl,N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro,chloro, bromo, and cyano; Y⁰ is selected from the group consisting of:1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷thiophene, 3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine,3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹ thiophene, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹furan, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ furan, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹pyrrole, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ pyrrole, 4-Q^(b)-2-Q^(s)-5-R¹⁹thiazole, and 2-Q^(b)-5-Q^(s)-4-R¹⁷ thiazole; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ areindependently selected from the group consisting of hydrido, methyl,ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl,1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio,ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;Q^(b) is NR²⁰R²¹ or C(NR²⁵)NR²³R²⁴; R²⁰, R²¹, R²³, R²⁴, and R²⁵ areindependently selected from the group consisting of hydrido, methyl, andethyl; Q^(s) is CH₂.
 28. Compound of claim 27 or a pharmaceuticallyacceptable salt thereof, wherein; J is selected from the groupconsisting of fluoro, trifluoromethyl, hydroxy, hydroxymethyl, amino,and aminomethyl; B is selected from the group consisting of2-aminophenyl, 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl,3-carboxyphenyl, 3-carboxy-5-hydroxyphenyl, 3-chlorophenyl,4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl,3,4-difluorophenyl, 3-hydroxyphenyl, 4-hydroxyphenyl,3-methoxyaminophenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl,4-methylphenyl, phenyl, 3-trifluoromethylphenyl, 2-imidazoyl, 2-pyridyl,3-pyridyl, 5-chloro-3-trifluoromethyl-2-pyridyl, 4-pyridyl, 2-thienyl,3-thienyl, and 3-trifluoromethyl-2-pyridyl; A is CH₂ or CH₂CH₂; X^(o) isselected from the group consisting of hydrido, hydroxy, amino, amidino,aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;R¹ is selected from the group consisting of hydrido, hydroxy,hydroxymethyl, amino, aminomethyl, cyano, methyl, trifluoromethyl, andfluoro; R² is selected from the group consisting of3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,3-amino-5-(N-benzylamidocarbonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-benzylamidosulfonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,3-amino-5-(N-ethylamidocarbonyl)phenyl,3-amino-5-(N-isopropylamidocarbonyl)phenyl,3-amino-5-(N-propylamidocarbonyl)phenyl,3-amino-5-(N-isobutylamidocarbonyl)phenyl,3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl,3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl,3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl,2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl,3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl,3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl,2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl,3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl,3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl,5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl,and 3-thienyl; Y⁰ is selected from the group consisting of:1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹thiophene, and 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene; R¹⁶ and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl,fluoro, chloro, and cyano; R¹⁷ and R¹⁸ are independently selected fromthe group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl,amino, carboxy, and cyano; Q^(b) is C(NR²⁵)NR²³R²⁴; R²³, R²⁴, and R²⁵are independently hydrido or methyl; Q^(s) is CH₂.
 29. Compound of claim28 or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of fluoro, hydroxy, hydroxymethyl, and amino;B is selected from the group consisting of 3-aminophenyl,3-amidinophenyl, 4-amidinophenyl, 3-chlorophenyl, 4-chlorophenyl,3,4-dichlorophenyl, 2-fluorophenyl, 4-methylphenyl, phenyl, 2-imidazoyl,3-pyridyl, 4-pyridyl, and 3-trifluoromethyl-2-pyridyl; A is CH₂ orCH₂CH₂; X^(o) is selected from the group consisting of hydrido, hydroxy,amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl,hydroxymethyl, and fluoro; R¹ is selected from the group consisting ofhydrido, hydroxy, hydroxymethyl, amino, aminomethyl, cyano, methyl,trifluoromethyl, and fluoro; R² is selected from the group consisting of3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-benzylamidosulfonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,3-amino-5-(N-ethylamidocarbonyl)phenyl,3-amino-5-(N-isopropylamidocarbonyl)phenyl,3-amino-5-(N-propylamidocarbonyl)phenyl,3-amino-5-(N-isobutylamidocarbonyl)phenyl,3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,3-carboxy-5-aminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl,3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl;Y⁰ is selected from the group consisting of 5-amidino-2-thienylmethyl,4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amdinobenzyl.30. Compound of claim 23 where said compound is selected from the groupof the Formula:

or a pharmaceutically acceptable salt thereof, wherein; R² is3-aminophenyl, B is phenyl, A is CH₂, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is chloro; R² is 3-aminophenyl, B is 3-chlorophenyl, A isCH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is phenyl, A is CH₂, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is hydrido; R² is 3-aminophenyl, B is 2-imidazoyl, A isCH₂CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 3-chlorophenyl, A isCH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is 3-chlorophenyl,A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is 3-chlorophenyl,A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro; R² is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 3-chlorophenyl, A isCH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is 3-chlorophenyl,A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R²is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is hydrido; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is hydrido; R² is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH₂CH₂,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is 3-aminophenyl, Bis 3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, andR¹ is chloro; R² is 3-aminophenyl, B is phenyl, A is CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is 3-aminophenyl, Bis 2-imidazoyl, A is CH₂CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, andR¹ is chloro; R² is 3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl,A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R²is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 3-chlorophenyl, A isCH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is 3-chlorophenyl,A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R²is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro; R² is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 3-chlorophenyl, A isCH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is 3-chlorophenyl,A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R²is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is hydrido; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is3-chlorophenyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is hydrido; R² is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH₂CH₂,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH₂CH₂, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido.
 31. Compound of claim22 of the Formula:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of halo, haloalkyl, hydroxy, hydroxyalkyl,amino, aminoalkyl, cyano, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ is alkyl orhaloalkyl; B is selected from the group consisting of hydrido, C2-C8alkyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein eachmember of group B is optionally substituted at any carbon up to andincluding 6 atoms from the point of attachment of B to A with one ormore of the group consisting of R³², R³³, R³⁴, R³⁵, and R³⁶; R³², R³³,R³⁴, R³⁵, and R³⁶ are independently selected from the group consistingof hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy,hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl,alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl,carboalkoxy, carboxy, carboxamido, cyano, and Q^(b); A is a bond or(CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is 0 or 1, pa is an integer selectedfrom 0 through 3, and W⁷ is (R⁷)NC(O) or N(R⁷); R⁷ is selected from thegroup consisting of hydrido, hydroxy and alkyl; R¹⁵ is selected from thegroup consisting of hydrido, halo, alkyl, and haloalkyl; R¹ and X^(o)are independently selected from the group consisting of hydrido,hydroxy, hydroxyamino, amidino, amino, cyano, hydroxyalkyl, alkoxy,alkyl, alkylamino, aminoalkyl, alkylthio, alkoxyamino, haloalkyl,haloalkoxy, and halo; R² is Z⁰-Q; Z⁰ is selected from the groupconsisting of a bond, CH₂, CH₂CH₂, W⁰—(CH(R⁴²))_(p) wherein p is 0 or 1and W⁰ is selected from the group consisting of O, S, and N(R⁴¹); R⁴¹and R⁴² are independently hydrido or alkyl; Q is phenyl or a heteroarylof 5 or 6 ring members, wherein a carbon adjacent to the carbon at thepoint of attachment of said phenyl or heteroaryl ring to Z⁰ isoptionally substituted by R⁹, the other carbon adjacent to the carbon atthe point of attachment is optionally substituted by R¹³, a carbonadjacent to R⁹ and two atoms from the carbon at the point of attachmentis optionally substituted by R¹⁰, a carbon adjacent to R¹³ and two atomsfrom the carbon at the point of attachment is optionally substituted byR¹², and any carbon adjacent to both R¹⁰ and R¹² is optionallysubstituted by R¹¹; R⁹, R¹¹, and R¹³ are independently selected from thegroup consisting of hydrido, hydroxy, amino, amidino, guanidino,alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl,amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl,hydroxyhaloalkyl, carboxy, carboxamido, and cyano; R¹⁰ and R¹² areindependently selected from the group consisting of hydrido, acetamido,haloacetamido, amidino, guanidino, alkyl, aryl, aralkyl, cycloalkyl,cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy,cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy,heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino,alkylamino, arylamino, aralkylamino, heteroarylamino,heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino,alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl,cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl,cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl,aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo,haloalkyl, and cyano; Y⁰ is phenyl or a heteroaryl of 5 or 6 ringmembers, wherein one carbon of said phenyl or said heteroaryl issubstituted by Q^(s), a carbon two or three atoms from the point ofattachment of Q^(s) to said phenyl or said heteroaryl is substituted byQ^(b), a carbon adjacent to the point of attachment of Q^(s) isoptionally substituted by R¹⁷, another carbon adjacent to the point ofattachment of Q^(s) is optionally substituted by R¹⁸, a carbon adjacentto Q^(b) is optionally substituted by R¹⁶, and another carbon adjacentto Q^(b) is optionally substituted by R¹⁹; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino,alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl,halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano; R¹⁶ orR¹⁹ is optionally selected from the group consisting of NR²⁰R²¹,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the proviso that R¹⁶,R¹⁹, and Q^(b) are not simultaneously hydrido; Q^(b) is selected fromthe group consisting of NR²⁰R²¹, hydrido, C(NR²⁵)NR²³R²⁴, andN(R²⁶)C(NR²⁵)N(R²³)(R²⁴), with the proviso that no more than one of R²⁰and R²¹ is hydroxy at the same time and with the further proviso that nomore than one of R²³ and R²⁴ is hydroxy at the same time; R²⁰, R²¹, R²³,R²⁴, R²⁵, and R²⁶ are independently selected from the group consistingof hydrido, alkyl, and hydroxy; Q^(s) is selected from the groupconsisting of a bond, CH₂, and CH₂CH₂.
 32. Compound of claim 31 or apharmaceutically acceptable salt thereof, wherein; J is selected fromthe group consisting of fluoro, chloro, trifluoromethyl, hydroxy,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl,amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, methoxy,trifluoromethoxy, N-methylamino, methythio, and trifluoromethylthio; Bis selected from the group consisting of hydrido, ethyl, 2-propynyl,2-propenyl, propyl, isopropyl, butyl, 2-butenyl, 3-butenyl, 2-butynyl,sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl,3-pentenyl, 4-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl,1-methyl-2-butenyl, 1-methyl-3-butenyl, 1-methyl-2-butynyl, 3-pentyl,1-ethyl-2-propenyl, 2-methylbutyl, 2-methyl-2-butenyl,2-methyl-3-butenyl, 2-methyl-3-butynyl, 3-methylbutyl,3-methyl-2-butenyl, 3-methyl-3-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl,4-hexenyl, 5-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl,1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl,1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl,1-ethyl-3-butenyl, 1-propyl-2-propenyl, 1-ethyl-2-butynyl, 1-heptyl,2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 2-heptynyl,3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl,1-methyl-3-hexenyl, 1-methyl-4-hexenyl, 1-methyl-5-hexenyl,1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methylhexynyl, 3-heptyl,1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-4-pentenyl,1-butyl-2-propenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl,2,2,2-trifluoroethyl, 2,2-difluoropropyl,4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl,5,5,6,6,6-pentafluorohexyl, and 3,3,3-trifluoropropyl, wherein eachmember of group B is optionally substituted at any carbon up to andincluding 5 atoms from the point of attachment of B to A with one ormore of the group consisting of R³², R³³, R³⁴, R³⁵, and R³⁶; R³², R³³,R³⁴, R³⁵, and R³⁶ are independently selected from the group consistingof hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy,propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido,trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino,methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, cyano, and Q^(b); A is selected from thegroup consisting of bond, NH, N(CH₃), N(OH), CH₂, CH₃CH, CF₃CH, NHC(O),N(CH₃)C(O), C(O)NH, C(O)N(CH₃), CH₂CH₂, CH₂CH₂CH₂, CH₃CHCH₂, andCF₃CHCH₂; R¹ and X^(o) are independently selected from the groupconsisting of hydrido, hydroxy, amino, amidino, hydroxyamino,aminomethyl, 1-aminoethyl, methylamino, dimethylamino, cyano, methyl,ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methoxyamino, methylthio,ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro,and bromo; R² is Z⁰-Q; Z⁰ is selected from the group consisting of abond, CH₂, CH₂CH₂, O, S, NH, N(CH₃), OCH₂, SCH₂, N(H)CH₂, and N(CH₃)CH₂;Q is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl,2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl,3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl,2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl,4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and1,3,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the pointof attachment of said phenyl or heteroaryl ring to Z⁰ is optionallysubstituted by R⁹, the other carbon adjacent to the carbon at the pointof attachment is optionally substituted by R¹³, a carbon adjacent to R⁹and two atoms from the carbon at the point of attachment is optionallysubstituted by R¹⁰, a carbon adjacent to R¹³ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹², andany carbon adjacent to both R¹⁰ and R¹² is optionally substituted byR¹¹; R⁹, R¹¹, and R¹³ are independently selected from the groupconsisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl,propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio,isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano; R¹⁰ and R¹² are independentlyselected from the group consisting of hydrido, amidino, guanidino,carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy,ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino,acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl,N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl,N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,N-(3-fluorobenzyl)amidocarbonyl,N-(2-trifluoromethylbenzyl)amidocarbonyl,N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl,N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl,N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy,cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy,cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy,3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino,5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl,4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino,4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy,4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl,5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy,2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy,3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy,2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy,3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy,3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy,3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy,4-fluorobenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy,3-fluoro-5-trifluoromethylbenzyloxy,4-fluoro-2-trifluoromethylbenzyloxy,4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy,2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy,4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy,4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy,4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy,4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino,1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino,phenylsulfonyl, 3-trifluoromethoxybenzyloxy,4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy,4-trifluoromethoxyphenoxy, 3-trifluoromethylbenzyloxy,4-trifluoromethylbenzyloxy, 2,4-bis-trifluoromethylbenzyloxy,3-trifluoromethylbenzyl, 3,5-bis-trifluoromethylbenzyloxy,4-trifluoromethylphenoxy, 3-trifluoromethylphenoxy,3-trifluoromethylthiobenzyloxy, 4-trifluoromethylthiobenzyloxy,2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy,3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and3-trifluoromethylthiophenoxy; Y⁰ is selected from the group consistingof: 3-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine, 2-Q^(b)-5-Q^(s)-3-R¹⁶-6-R¹⁸pyrazine, 3-Q^(b)-5-Q^(s)-2-R¹⁸-5-R¹⁸-4-R¹⁹ pyridazine,2-Q^(b)-5-Q^(s)-4-R¹⁷-6-R¹⁸ pyrimidine, 5-Q^(b)-2-Q^(s)-4-R¹⁶-6-R¹⁹pyrimidine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹ thiophene,2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹furan, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ furan, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹pyrrole, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ pyrrole, 4-Q^(b)-2-Q^(s)-5-R¹⁹imidazole, 2-Q^(b)-4-Q^(s)-5-R¹⁷ imidazole, 3-Q^(b)-5-Q^(s)-4-R¹⁶isoxazole, 5-Q^(b)-3-Q^(s)-4-R¹⁶ isoxazole, 2-Q^(b)-5-Q^(s)-4-R¹⁶pyrazole, 4-Q^(b)-2-Q^(s)-5-R¹⁹ thiazole, and 2-Q^(b)-5-Q^(s)-4-R¹⁷thiazole; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from thegroup consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy,amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy,amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio,trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl,ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, and cyano; R¹⁶ or R¹⁹ is optionallyselected from the group consisting of NR²⁰R²¹, C(NR²⁵)NR²³R²⁴, andN(R²⁶)C(NR²⁵)N(R²³)(R²⁴), with the proviso that R¹⁶, R¹⁹, and Q^(b) arenot simultaneously hydrido; Q^(b) is selected from the group consistingof NR²⁰R²¹, hydrido, C(NR²⁵)NR²³R²⁴, and N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), withthe proviso that no more than one of R²⁰ and R²¹ is hydroxy at the sametime and with the further proviso that no more than one of R²³ and R²⁴is hydroxy at the same time; R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ areindependently selected from the group consisting of hydrido, methyl,ethyl, propyl, butyl, isopropyl, and hydroxy; Q^(s) is selected from thegroup consisting of a bond, CH₂, and CH₂CH₂.
 33. Compound of claim 32 ora pharmaceutically acceptable salt thereof, wherein; J is selected fromthe group consisting of fluoro, chloro, trifluoromethyl, hydroxy,hydroxymethyl, amino, aminomethyl, methoxy, trifluoromethoxy, andN-methylamino; B is selected from the group consisting of hydrido,ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl,(R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl,2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl,4-methyl-2-pentyl, 3-hydroxypropyl, 1-methoxy-2-propyl, 2-methoxyethyl,2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl,6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl,3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl,6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl,(S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl; A isselected from the group consisting of a bond, CH₂, NHC(O), CH₂CH₂,CH₂CH₂CH₂, and CH₃CHCH₂; R¹ and X^(o) are independently selected fromthe group consisting of hydrido, hydroxy, amino, amidino, hydroxyamino,aminomethyl, methylamino, cyano, methyl, trifluoromethyl, methoxy,hydroxymethyl, methoxyamino, methylthio, trifluoromethoxy, fluoro, andchloro; R² is Z⁰-Q; Z⁰ is selected from the group consisting of a bond,CH₂, O, S, NH, N(CH₃), OCH₂, and SCH₂; Q is selected from the groupconsisting of 3-amidocarbonyl-5-aminophenyl,3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-benzylphenyl,3-amino-5-(2-phenylethyl)phenyl, 3-amino-5-benzylaminophenyl,3-amino-5-(2-phenylethylamino)phenyl, 3-amino-5-benzyloxyphenyl,3-amino-5-(2-phenylethoxy)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-benzylamidosulfonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,3-amino-5-(N-ethylamidocarbonyl)phenyl,3-amino-5-(N-isopropylamidocarbonyl)phenyl,3-amino-5-(N-propylamidocarbonyl)phenyl,3-amino-(N-isobutylamidocarbonyl)phenyl,3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,3-aminophenyl, 3-amino-5-(4-trifluoromethylbenzylamino)phenyl,3-amino-5-(4-trifluoromethylbenzyloxy)phenyl, 3-carboxyphenyl,3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl,2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,2-fluorophenyl, 3-fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl,3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl,phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; Y⁰ isselected from the group consisting of:1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹thiophene, and 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene; R¹⁶ and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl,fluoro, chloro, and cyano; R¹⁶ or R¹⁹ is optionally C(NR²⁵)NR²³R²⁴ withthe proviso that R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido; R¹⁷and R¹⁸ are independently selected from the group consisting of hydrido,fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano; Q^(b)is C(NR²⁵)NR²³R²⁴ or hydrido; R²³, R²⁴, and R²⁵ are independentlyhydrido or methyl; Q^(s) is CH₂.
 34. Compound of claim 31 of theFormula:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of halo, haloalkyl, hydroxy, hydroxyalkyl,amino, and aminoalkyl; B is selected from the group consisting ofhydrido, C2-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl,wherein each member of group B is optionally substituted at any carbonup to and including 6 atoms from the point of attachment of B to A withone or more of the group consisting of R³², R³³, R³⁴, R³⁵, and R³⁶; R³²,R³³, R³⁴, R³⁵, and R³⁶ are independently selected from the groupconsisting of hydrido, acetamido, haloacetamido, amidino, guanidino,alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio,amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl,carboalkoxy, carboxy, carboxamido, cyano, and Q^(b); A is a bond or(CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is 0 or 1, pa is an integer selectedfrom 0 through 3, and W⁷ is N(R⁷); R⁷ is hydrido or alkyl; R¹⁵ isselected from the group consisting of hydrido, halo, alkyl, andhaloalkyl; R¹ and X^(o) are independently selected from the groupconsisting of hydrido, hydroxy, hydroxyamino, amidino, amino, cyano,hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio,alkoxyamino, haloalkyl, haloalkoxy, and halo; R² is Z⁰-Q; Z⁰ is a bond;Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbonadjacent to the carbon at the point of attachment of said phenyl orheteroaryl ring to Z⁰ is optionally substituted by R⁹, the other carbonadjacent to the carbon at the point of attachment is optionallysubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹⁰, acarbon adjacent to R¹³ and two atoms from the carbon at the point ofattachment is optionally substituted by R¹², and any carbon adjacent toboth R¹⁰ and R¹² is optionally substituted by R¹¹; R⁹, R¹¹, and R¹³ areindependently selected from the group consisting of hydrido, hydroxy,amino, amidino, guanidino, alkylamino, alkylthio, alkoxy, alkylsulfinyl,alkylsulfonyl, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy,hydroxyalkyl, carboxy, carboxamido, and cyano; R¹⁰ and R¹² areindependently selected from the group consisting of hydrido, acetamido,haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, hydroxy,amino, alkylamino, alkylsulfonamido, amidosulfonyl, hydroxyalkyl,aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxamido,carboxyalkyl, and cyano; Y⁰ is phenyl or a heteroaryl of 5 or 6 ringmembers, wherein one carbon of said phenyl or said heteroaryl issubstituted by Q^(s), a carbon two or three atoms from the point ofattachment of Q^(s) to said phenyl or said heteroaryl is substituted byQ^(b), a carbon adjacent to the point of attachment of Q^(s) isoptionally substituted by R¹⁷, another carbon adjacent to the point ofattachment of Q^(s) is optionally substituted by R¹⁸, a carbon adjacentto Q^(b) is optionally substituted by R¹⁶, and another carbon adjacentto Q^(b) is optionally substituted by R¹⁹; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino,alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl,halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano; R¹⁶ orR¹⁹ is optionally selected from the group consisting of NR²⁰R²¹,N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), and C(NR²⁵)NR²³R²⁴, with the proviso that R¹⁶,R¹⁹, and Q^(b) are not simultaneously hydrido; Q^(b) is selected fromthe group consisting of NR²⁰R²¹, hydrido, N(R²⁶)C(NR²⁵)N(R²³)(R²⁴), andC(NR²⁵)NR²³R²⁴; R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ are independentlyhydrido or alkyl; Q^(s) is CH₂.
 35. Compound of claim 34 or apharmaceutically acceptable salt thereof, wherein; J is selected fromthe group consisting of fluoro, chloro, trifluoromethyl, hydroxy,hydroxymethyl, amino, and aminomethyl; B is selected from the groupconsisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl,butyl, 2-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl,2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 2-pentynyl,3-pentynyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 2-methyl-2-butenyl,3-methylbutyl, 3-methyl-2-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl,4-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl,1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-2-pentynyl,1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-heptyl, 2-heptenyl,3-heptenyl, 4-heptenyl, 5-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl,5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl,1-methyl-4-hexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl,1-methylhexynyl, 3-heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl,1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl,2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl,4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and3,3,3-trifluoropropyl, wherein each member of group B is optionallysubstituted at any carbon up to and including 5 atoms from the point ofattachment of B to A with one or more of the group consisting of R³²,R³³, R³⁴, R³⁵, and R³⁶; R³², R³³, R³⁴, R³⁵, and R³⁶ are independentlyselected from the group consisting of hydrido, amidino, guanidino,methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino,dimethylamino, methoxyamino, methylthio, ethylthio, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo,amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl,carboxy, cyano, and Q^(b); A is selected from the group consisting of abond, NH, N(CH₃), CH₂, CH₃CH, and CH₂CH₂; A is optionally selected fromthe group consisting of CH₂N(CH₃), CH₂N(CH₂CH₃), CH₂CH₂N(CH₃), andCH₂CH₂N(CH₂CH₃) with the proviso that B is hydrido; X^(o) is selectedfrom the group consisting of hydrido, hydroxy, amino, amidino,aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, chloro, andfluoro; R¹ is selected from the group consisting of hydrido, hydroxy,hydroxymethyl, amino, aminomethyl, methylamino, cyano, methyl,trifluoromethyl, methoxy, methylthio, trifluoromethoxy, fluoro, andchloro; R² is selected from the group consisting of phenyl, 2-thienyl,2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl,and 3-pyridyl, wherein a carbon adjacent to the carbon at the point ofattachment of said phenyl or heteroaryl ring to the benzene ring isoptionally substituted by R⁹, the other carbon adjacent to the carbon atthe point of attachment is optionally substituted by R¹³, a carbonadjacent to R⁹ and two atoms from the carbon at the point of attachmentis optionally substituted by R¹⁰, a carbon adjacent to R¹³ and two atomsfrom the carbon at the point of attachment is optionally substituted byR¹², and any carbon adjacent to both R¹⁰ and R¹² is optionallysubstituted by R¹¹; R⁹, R¹¹, and R¹³ are independently selected from thegroup consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy,amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl,pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl,carboxy, and cyano; R¹⁰ and R¹² are independently selected from thegroup consisting of hydrido, amidino, amidocarbonyl,N-methylamidocarbonyl, N-benzylamidocarbonyl,N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl,N-(2-trifluoromethylbenzyl)amidocarbonyl,N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl,N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl,N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy,hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy,carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino,dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl,N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro,chloro, bromo, and cyano; Y⁰ is selected from the group consisting of:1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷thiophene, 3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine,3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹ thiophene, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹furan, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ furan, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹pyrrole, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ pyrrole, 4-Q^(b)-2-Q^(s)-5-R¹⁹thiazole, and 2-Q^(b)-5-Q^(s)-4-R¹⁷ thiazole; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ areindependently selected from the group consisting of hydrido, methyl,ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl,1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio,ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;Q^(b) is selected from the group consisting of NR²⁰R²¹, C(NR²⁵)NR²³R²⁴,and N(R²⁶)C(NR²⁵)N(R²³)(R²⁴); R²⁰, R²¹, R²³, R²⁴, R²⁵, and R²⁶ areindependently selected from the group consisting of hydrido, methyl, andethyl; Q^(s) is CH₂.
 36. Compound of claim 35 or a pharmaceuticallyacceptable salt thereof, wherein; J is selected from the groupconsisting of fluoro, trifluoromethyl, hydroxy, hydroxymethyl, amino,and aminomethyl; B is selected from the group consisting of hydrido,ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl,(R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl,2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl,4-methyl-2-pentyl, 3-hydroxypropyl, 1-methoxy-2-propyl, 2-methoxyethyl,2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl,6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl,3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl,6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl,(S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl; A isselected from the group consisting of a bond, CH₂, CH₃CH, and CH₂CH₂;X^(o) is selected from the group consisting of hydrido, hydroxy, amino,amidino, aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, andfluoro; R¹ is selected from the group consisting of hydrido, hydroxy,hydroxymethyl, amino, aminomethyl, cyano, methyl, trifluoromethyl, andfluoro; R² is selected from the group consisting of3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,3-amino-5-(N-benzylamidocarbonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-benzylamidosulfonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,3-amino-5-(N-ethylamidocarbonyl)phenyl,3-amino-5-(N-isopropylamidocarbonyl)phenyl,3-amino-(N-propylamidocarbonyl)phenyl,3-amino-(N-isobutylamidocarbonyl)phenyl,3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl,3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl,3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl,2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl,3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl,3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl,2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl,3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl,3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl,5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl,and 3-thienyl; Y⁰ is selected from the group consisting of:1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹thiophene, and 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene; R¹⁶ and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl,fluoro, chloro, and cyano; R¹⁷ and R¹⁸ are independently selected fromthe group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl,amino, carboxy, and cyano; Q^(b) is C(NR²⁵)NR²³R²⁴; R²³, R²⁴, and R²⁵are independently hydrido or methyl; Q^(s) is CH₂.
 37. Compound of claim36 or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of fluoro, hydroxy, hydroxymethyl, and amino;B is selected from the group consisting of hydrido, ethyl, 2-propenyl,2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl,tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl,2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-pentyl,3-hydroxypropyl, 1-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl,3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl,2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl,4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl,2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl,3-aminopropyl, 2-hexyl, and 4-aminobutyl; A is selected from the groupconsisting of a bond, CH₂, CH₃CH, and CH₂CH₂; X^(o) is selected from thegroup consisting of hydrido, hydroxy, amino, amidino, aminomethyl,cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro; R¹ isselected from the group consisting of hydrido, hydroxy, hydroxymethyl,amino, aminomethyl, cyano, methyl, trifluoromethyl, and fluoro; R² isselected from the group consisting of 3-amidocarbonyl-5-aminophenyl,3-amino-5-(N-benzylamidocarbonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-benzylamidosulfonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,3-amino-5-(N-ethylamidocarbonyl)phenyl,3-amino-5-(N-isopropylamidocarbonyl)phenyl,3-amino-5-(N-propylamidocarbonyl)phenyl,3-amino-5-(N-isobutylamidocarbonyl)phenyl,3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,3-carboxy-5-aminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl,3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl;Y⁰ is selected from the group consisting of 5-amidino-2-thienylmethyl,4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amidinobenzyl.38. Compound of claim 31 where said compound is selected from the groupof the Formula:

or a pharmaceutically acceptable salt thereof, wherein; R² is3-aminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is 3-aminophenyl, Bis (S)-2-butyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro; R² is 5-amino-2-fluorophenyl, B is isopropyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is2-methyl-3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is 3-aminophenyl, Bis ethyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-aminophenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3-aminophenyl, B is 2-propenyl, A is a bond, Y⁰ is 4-amidinobenzyl, J ishydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is isopropyl, A is abond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R²is 3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, Jis hydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is 2-butyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-aminophenyl, B is (R)-2-butyl, A is a bond, Y⁰ is 4-amidinobenzyl, Jis hydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is 2-propynyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-aminophenyl, B is 3-pentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J ishydroxy, and R¹ is hydrido; R² is 3-aminophenyl, B is hydrido, A is CH₂,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-aminophenyl, B is ethyl, A is CH₂, Y⁰ is 4-amidinobenzyl, J ishydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is 2-methypropyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-aminophenyl, B is 2-propyl, A is CH₃CH, Y⁰ is 4-amidinobenzyl, J ishydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is propyl, A is abond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R²is 3-aminophenyl, B is 6-amidocarbonylhexyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is 3-aminophenyl, Bis tert-butyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is hydrido; R² is 3-aminophenyl, B is tert-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is 3-aminophenyl, Bis 3-hydroxypropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy,and R¹ is chloro; R² is 3-aminophenyl, B is 2-methylpropyl, A is a bond,Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3-aminophenyl, B is butyl, A is a bond, Y⁰ is 4-amidinobenzyl, J ishydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is 1-methoxy-2-propyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R²is 3-aminophenyl, B is 2-methoxyethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is 3-aminophenyl, Bis 2-propyl, A is a bond, Y⁰ is 5-amidino-2-thienylmethyl, J is hydroxy,and R¹ is chloro; R² is 5-amino-2-methylthiophenyl, B is 2-propyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-carbomethoxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is 3-aminophenyl, Bis isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is bromo; R² is 3-amino-5-carboxamidophenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-benzyl-N-methylamidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(2-phenyl-2-propyl)amidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(2,4-dichlorobenzyl)amidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(4-bromobenzyl)amidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is isopropyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is3-amino-5-(N-(3-trifluoromethylbenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-amino-5-(N-isobutylamidocarbonyl)phenyl, B is isopropyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R²is 3-amino-5-(N-cyclobutylamidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-cyclopentylamidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-cycloheptylamidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(2-pyridylmethyl)amidocarbonyl)phenyl, B is isopropyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(3-pyridylmethyl)amidocarbonyl)phenyl, B is isopropyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(2-(4-methoxyphenyl)ethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-amino-5-(N-(3-phenylpropyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-amino-5-(N-(2,2-diphenylethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-amino-5-(N-(2-naphthylmethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is3-amino-5-(N-(1,2,3,4-tetrahydronaphth-2-ylmethyl)amidocarbonyl)phenyl,B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹is chloro; R² is 3-aminophenyl, B is 2-propyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is hydrido; R² is3-carboxyphenyl, B is 2-propyl, A is a bond, Y⁰ is 4-amidinobenzyl, J ishydroxy, and R¹ is hydrido; R² is 3-aminophenyl, B is 2-propyl, A is abond, Y⁰ is 4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro; R²is 3,5-diaminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3,5-diaminophenyl, B is (S)-2-butyl, A is a bond, Y⁰ is 4-amidinobenzyl,J is hydroxy, and R¹ is chloro; R² is 3,5-diaminophenyl, B is isopropyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R²is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzylbenzyl, J is hydroxy, and R¹ is chloro; R² is3,5-diaminophenyl, B is ethyl, A is a bond, Y⁰ is 4-amidinobenzyl, J ishydroxy, and R¹ is chloro; R² is 3,5-diaminophenyl, B is ethyl, A is abond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R²is 3-amino-5-carboxyphenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y⁰is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is (S)-2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzylbenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is ethyl, A is a bond, Y⁰ is 4-amidinobenzyl,J is hydroxy, and R¹ is chloro; R² is 3-amino-5-carboxyphenyl, B isethyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹is chloro; R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is2,2,2-trifluoroethyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy,and R¹ is chloro; R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is(S)-2-butyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidino-2-fluorobenzylbenzyl, J is hydroxy, and R¹ ischloro; R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzylbenzyl, J is hydroxy, and R¹ is hydrido; R² is3-aminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is 3-aminophenyl, Bis (S)-2-butyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro; R² is 5-amino-2-fluorophenyl, B is isopropyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is2-methyl-3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is 3-aminophenyl, Bis ethyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is 3-aminophenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is 2-propenyl, A is a bond, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is chloro; R² is 3-aminophenyl, B is isopropyl, A is abond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R²is 3-aminophenyl, B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, Jis fluoro, and R¹ is chloro; R² is 3-aminophenyl, B is 2-butyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is (R)-2-butyl, A is a bond, Y⁰ is 4-amidinobenzyl, Jis fluoro, and R¹ is chloro; R² is 3-aminophenyl, B is 2-propynyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is 3-pentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is hydrido; R² is 3-aminophenyl, B is hydrido, A is CH₂,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is ethyl, A is CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro,and R¹ is chloro; R² is 3-aminophenyl, B is 2-methypropyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is 2-propyl, A is CH₃CH, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is chloro; R² is 3-aminophenyl, B is propyl, A is a bond,Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is 6-amidocarbonylhexyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is 3-aminophenyl, Bis tert-butyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is hydrido; R² is 3-aminophenyl, B is tert-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is 3-aminophenyl, Bis 3-hydroxypropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, andR¹ is chloro; R² is 3-aminophenyl, B is 2-methylpropyl, A is a bond, Y⁰is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is butyl, A is a bond, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is chloro; R² is 3-aminophenyl, B is 1-methoxy-2-propyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is 2-methoxyethyl, A is a bond, Y⁰ is 4-amidinobenzyl,J is fluoro, and R¹ is chloro; R² is 3-aminophenyl, B is 2-propyl, A isa bond, Y⁰ is 5-amidino-2-thienylmethyl, J is fluoro, and R¹ is chloro;R² is 5-amino-2-methylthiophenyl, B is 2-propyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-carbomethoxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is 3-aminophenyl, Bis isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ isbromo; R² is 3-amino-5-carboxamidophenyl, B is isopropyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzyl-N-methylamidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-phenyl-2-propyl)amidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2,4-dichlorobenzyl)amidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(4-bromobenzyl)amidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is isopropyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is 3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is3-amino-5-(N-(3-trifluoromethylbenzyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is 3-amino-5-(N-isobutylamidocarbonyl)phenyl, B is isopropyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-cyclobutylamidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-cyclopentylamidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-cycloheptylamidocarbonyl)phenyl, B is isopropyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-pyridylmethyl)amidocarbonyl)phenyl, B is isopropyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(3-pyridylmethyl)amidocarbonyl)phenyl, B is isopropyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-(4-methoxyphenyl)ethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is 3-amino-5-(N-(3-phenylpropyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is 3-amino-5-(N-(2,2-diphenylethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is 3-amino-5-(N-(2-naphthylmethyl)amidocarbonyl)phenyl, B isisopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is3-amino-5-(N-(1,2,3,4-tetrahydronaphth-2-ylmethyl)amidocarbonyl)phenyl,B is isopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹is chloro; R² is 3-aminophenyl, B is 2-propyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is hydrido; R² is3-carboxyphenyl, B is 2-propyl, A is a bond, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is hydrido; R² is 3-aminophenyl, B is 2-propyl, A is abond, Y⁰ is 4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is chloro; R²is 3,5-diaminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is 3,5-diaminophenyl,B is (S)-2-butyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, andR¹ is chloro; R² is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzylbenzyl, J is fluoro, and R¹ is chloro; R² is3,5-diaminophenyl, B is ethyl, A is a bond, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is chloro; R² is 3,5-diaminophenyl, B is ethyl, A is abond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R²is 3-amino-carboxyphenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is (S)-2-butyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzylbenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is ethyl, A is a bond, Y⁰ is 4-amidinobenzyl,J is fluoro, and R¹ is chloro; R² is 3-amino-5-carboxyphenyl, B isethyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹is chloro; R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is2,2,2-trifluoroethyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro,and R¹ is chloro; R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is(S)-2-butyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, Ais a bond, Y⁰ is 4-amidino-2-fluorobenzylbenzyl, J is fluoro, and R¹ ischloro; R² is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3,5-diaminophenyl, B is isopropyl, A is a bond, Y⁰ is4-amidinobenzylbenzyl, J is fluoro, and R¹ is hydrido.
 39. Compound ofclaim 22 of the Formula:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of halo, haloalkyl, hydroxy, hydroxyalkyl,amino, aminoalkyl, cyano, O—R⁶, NH—R⁶, and S—R⁶, wherein R⁶ is alkyl orhaloalkyl; B is a C3-C7 cycloalkyl or a C4-C6 saturated heterocyclyl,wherein each ring carbon is optionally substituted with R³³, a ringcarbon other than the ring carbon at the point of attachment of B to Ais optionally substituted with oxo provided that no more than one ringcarbon is substituted by oxo at the same time, ring carbons and anitrogen adjacent to the carbon atom at the point of attachment areoptionally substituted with R⁹ or R¹³, a ring carbon or nitrogenadjacent to the R⁹ position and two atoms from the point of attachmentis optionally substituted with R¹⁰, a ring carbon or nitrogen adjacentto the R¹³ position and two atoms from the point of attachment isoptionally substituted with R¹², a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹⁰ position isoptionally substituted with R¹¹, a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹² position isoptionally substituted with R³³, and a ring carbon or nitrogen fouratoms from the point of attachment and adjacent to the R¹¹ and R³³positions is optionally substituted with R³⁴; R⁹, R¹¹, and R¹³ areindependently selected from the group consisting of hydrido, hydroxy,amino, amidino, guanidino, alkylamino, alkylthio, alkylsulfonamido,alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, alkoxy, halo,haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboxy,carboxamido, and cyano; R¹⁰ and R¹² are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl,heteroaryl, heterocyclyl, alkoxy, cycloalkoxy, cycloalkylalkoxy,aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy, heterocyclyloxy,heterocyclylalkoxy, hydroxy, amino, alkoxyamino, alkylamino, arylamino,aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino,heterocyclylalkylamino, alkylsulfonamido, amidosulfonyl, arylsulfinyl,aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl,aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl,hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl,carboxamido, halo, haloalkyl, and cyano; R³³ and R³⁴ are independentlyselected from the group consisting of hydrido, acetamido, haloacetamido,amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino,alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy,hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, andcyano; R³³ is optionally Q^(b); A is a bond or (CH(R¹⁵))_(pa)—(W⁷)_(rr)wherein rr is 0 or 1, pa is an integer selected from 0 through 3, and W⁷is (R⁷)NC(O) or N(R⁷); R⁷ is selected from the group consisting ofhydrido, hydroxy and alkyl; R¹⁵ is selected from the group consisting ofhydrido, halo, alkyl, and haloalkyl; R¹ and X^(o) are independentlyselected from the group consisting of hydrido, hydroxy, hydroxyamino,amidino, amino, cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino,aminoalkyl, alkylthio, alkoxyamino, haloalkyl, haloalkoxy, and halo; R²is Z⁰-Q; Z⁰ is selected from the group consisting of a bond, CH₂,CH₂CH₂, W⁰—(CH(R⁴²))_(p) wherein p is 0 or 1 and W⁰ is selected from thegroup consisting of O, S, and N(R⁴¹); R⁴¹ and R⁴² are independentlyhydrido or alkyl; Q is phenyl or a heteroaryl of 5 or 6 ring members,wherein a carbon adjacent to the carbon at the point of attachment ofsaid phenyl or heteroaryl ring to Z⁰ is optionally substituted by R⁹,the other carbon adjacent to the carbon at the point of attachment isoptionally substituted by R¹³, a carbon adjacent to R⁹ and two atomsfrom the carbon at the point of attachment is optionally substituted byR¹⁰, a carbon adjacent to R¹³ and two atoms from the carbon at the pointof attachment is optionally substituted by R¹², and any carbon adjacentto both R¹⁰ and R¹² is optionally substituted by R¹¹; Y⁰ is phenyl or aheteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl orsaid heteroaryl is substituted by Q^(s), a carbon two or three atomsfrom the point of attachment of Q^(s) to said phenyl or said heteroarylis substituted by Q^(b), a carbon adjacent to the point of attachment ofQ^(s) is optionally substituted by R¹⁷, another carbon adjacent to thepoint of attachment of Q^(s) is optionally substituted by R¹⁸, a carbonadjacent to Q^(b) is optionally substituted by R¹⁶, and another carbonadjacent to Q^(b) is optionally substituted by R¹⁹; R¹⁶, R¹⁷, R¹⁸, andR¹⁹ are independently selected from the group consisting of hydrido,amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino,alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl,haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl,aminoalkyl, and cyano; R¹⁶ or R¹⁹ is optionally NR²⁰R²¹ or andC(NR²⁵)NR²³R²⁴, with the proviso that R¹⁶, R¹⁹, and Q^(b) are notsimultaneously hydrido; Q^(b) is selected from the group consisting ofNR²⁰R²¹, hydrido, and C(NR²⁵)NR²³R²⁴, with the proviso that no more thanone of R²⁰ and R²¹ is hydroxy at the same time and with the furtherproviso that no more than one of R²³ and R²⁴ is hydroxy at the sametime; R²⁰, R²¹, R²³, R²⁴, and R²⁵ are independently selected from thegroup consisting of hydrido, alkyl, and hydroxy; Q^(s) is selected fromthe group consisting of a bond, CH₂, and CH₂CH₂.
 40. Compound of claim39 or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of fluoro, chloro, trifluoromethyl, hydroxy,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl,amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, methoxy,trifluoromethoxy, N-methylamino, methythio, and trifluoromethylthio; Bis selected from the group consisting of cyclopropyl, cyclobutyl,oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, thiaetan-3-yl,cyclopentyl, cyclohexyl, norbornyl, 7-oxabicyclo[2.2.1]heptan-2-yl,bicyclo[3.1.0]hexan-6-yl, cycloheptyl, 2-morpholinyl, 3-morpholinyl,4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl,2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl,2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl, 4H-2-pyranyl, 4H-3-pyranyl,4H-4-pyranyl, 4H-pyran-4-one-2-yl, 4H-pyran-4-one-3-yl,2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydropyranyl,3-tetrahydropyranyl, 4-tetrahydropyranyl, 2-tetrahydrothienyl, and3-tetrahydrothienyl, wherein each ring carbon is optionally substitutedwith R³³, ring carbons and a nitrogen adjacent to the carbon atom at thepoint of attachment are optionally substituted with R⁹ or R¹³, a ringcarbon or nitrogen adjacent to the R⁹ position and two atoms from thepoint of attachment is optionally substituted with R¹⁰, and a ringcarbon or nitrogen adjacent to the R¹³ position and two atoms from thepoint of attachment is optionally substituted with R¹²; R⁹, R¹¹, and R¹³are independently selected from the group consisting of hydrido,amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy,ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino,N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, and cyano; R¹⁰ and R¹² are independentlyselected from the group consisting of hydrido, amidino, guanidino,carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy,ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino,acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl,N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido,amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl,N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,N-(3-fluorobenzyl)amidocarbonyl,N-(2-trifluoromethylbenzyl)amidocarbonyl,N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl,N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl,N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy,cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy,cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy,3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino,5-bromopyrid-2-ylmethyl amino, 4-butoxyphenamino, 3-chlorobenzyl,4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino,4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy,4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl,5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy,2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy,3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy,2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy,3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy,3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy,3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy,4-fluorobenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy,3-fluoro-5-trifluoromethylbenzyloxy,4-fluoro-2-trifluoromethylbenzyloxy,4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy,2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy,4-fluorophenylamino, 2-fluorotrifluoromethylphenoxy,4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy,4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy,4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino,1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino,phenylsulfonyl, 3-trifluoromethoxybenzyloxy,4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy,4-trifluoromethoxyphenoxy, 3-trifluoromethylbenzyloxy,4-trifluoromethylbenzyloxy, 2,4-bis-trifluoromethylbenzyloxy,3-trifluoromethylbenzyl, 3,5-bis-trifluoromethylbenzyloxy,4-trifluoromethylphenoxy, 3-trifluoromethylphenoxy,3-trifluoromethylthiobenzyloxy, 4-trifluoromethylthiobenzyloxy,2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy,3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and3-trifluoromethylthiophenoxy; R³³ is selected from the group consistingof hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy,propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido,trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino,methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl,methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,N,N-dimethylamidocarbonyl, cyano, and Q^(b); A is selected from thegroup consisting of a bond, NH, N(CH₃), N(OH), CH₂, CH₃CH, CF₃CH,NHC(O), N(CH₃)C(O), C(O)NH, C(O)N(CH₃), CH₂CH₂, CH₂CH₂CH₂, CH₃CHCH₂, andCF₃CHCH₂; R¹ and X^(o) are independently selected from the groupconsisting of hydrido, hydroxy, amino, amidino, hydroxyamino,aminomethyl, 1-aminoethyl, methylamino, dimethylamino, cyano, methyl,ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy,hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methoxyamino, methylthio,ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro,and bromo; R² is Z⁰-Q; Z⁰ is selected from the group consisting of abond, CH₂, CH₂CH₂, O, S, NH, N(CH₃), OCH₂, SCH₂, N(H)CH₂, and N(CH₃)CH₂;Q is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl,2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl,3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl,2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl,4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and1,3,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the pointof attachment of said phenyl or heteroaryl ring to Z⁰ is optionallysubstituted by R⁹, the other carbon adjacent to the carbon at the pointof attachment is optionally substituted by R¹³, a carbon adjacent to R⁹and two atoms from the carbon at the point of attachment is optionallysubstituted by R¹⁰, a carbon adjacent to R¹³ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹², andany carbon adjacent to both R¹⁰ and R¹² is optionally substituted byR¹¹; Y⁰ is selected from the group consisting of:1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine, 2-Q^(b)-5-Q^(s)-3-R¹⁶-6-R¹⁸pyrazine, 3-Q^(b)-6-Q^(s)-2-R¹⁸-5-R¹⁸-4-R¹⁹ pyridazine,2-Q^(b)-5-Q^(s)-4-R¹⁷-6-R¹⁸ pyrimidine, 5-Q^(b)-2-Q^(s)-4-R¹⁶-6-R¹⁹pyrimidine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹ thiophene,2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹furan, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ furan, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹pyrrole, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ pyrrole, 4-Q^(b)-2-Q^(s)-5-R¹⁹imidazole, 2-Q^(b)-4-Q^(s)-5-R¹⁷ imidazole, 3-Q^(b)-5-Q^(s)-4-R¹⁶isoxazole, 5-Q^(b)-3-Q^(s)-4-R¹⁶ isoxazole, 2-Q^(b)-5-Q^(s)-4-R¹⁶pyrazole, 4-Q^(b)-2-Q^(s)-5-R¹⁰ thiazole, and 2-Q^(b)-5-Q^(s)-4-R¹⁷thiazole; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from thegroup consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy,amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy,amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio,trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl,ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,2,2,3,3,3-pentafluoropropyl, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl,1-hydroxyethyl, 2-hydroxyethyl, and cyano; R¹⁶ or R¹⁹ is optionallyC(NR²⁵)NR²³R²⁴ with the proviso that R¹⁶, R¹⁹, and Q^(b) are notsimultaneously hydrido; Q^(b) is C(NR²⁵)NR²³R²⁴ or hydrido, with theproviso that no more than one of R²³ and R²⁴ is hydroxy at the sametime; R²³, R²⁴, and R²⁵ are independently selected from the groupconsisting of hydrido, methyl, ethyl, and hydroxy; Q^(s) is selectedfrom the group consisting of a bond, CH₂ and CH₂CH₂.
 41. Compound ofclaim 40 or a pharmaceutically acceptable salt thereof, wherein; J isselected from the group consisting of fluoro, chloro, trifluoromethyl,hydroxy, hydroxymethyl, amino, aminomethyl, methoxy, trifluoromethoxy,and N-methylamino; B is selected from the group consisting ofcyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, 1-pyrrolidinyl,1-piperidinyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl,7-oxabicyclo[2.2.1]heptan-2-yl, bicyclo[3.1.0]hexanyl, 2-morpholinyl,3-morpholinyl, 4-morpholinyl, 1-piperazinyl, 2-piperazinyl,1-piperidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl,1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl,4H-2-pyranyl, 4H-3-pyranyl, 4H-4-pyranyl, 4H-pyran-4-one-2-yl,4H-pyran-4-one-3-yl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl,2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl,2-tetrahydrothienyl, and 3-tetrahydrothienyl; A is selected from thegroup consisting of a bond, CH₂, NHC(O), CH₂CH₂, and CH₂CH₂CH₂; R¹ andX^(o) are independently selected from the group consisting of hydrido,hydroxy, amino, amidino, hydroxyamino, aminomethyl, methylamino, cyano,methyl, trifluoromethyl, methoxy, hydroxymethyl, methoxyamino,methylthio, trifluoromethoxy, fluoro, and chloro; R² is Z⁰-Q; Z⁰ isselected from the group consisting of a bond, CH₂, O, S, NH, N(CH₃),OCH₂, and SCH₂; Q is selected from the group consisting of3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl,3-amino-5-benzylphenyl, 3-amino-5-(2-phenylethyl)phenyl,3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenylethylamino)phenyl,3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-benzylamidosulfonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,3-amino-5-(N-ethylamidocarbonyl)phenyl,3-amino-5-(N-isopropylamidocarbonyl)phenyl,3-amino-5-(N-propylamidocarbonyl)phenyl,3-amino-5-(N-isobutylamidocarbonyl)phenyl,3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,3-aminophenyl, 3-amino-5-(4-trifluoromethylbenzylamino)phenyl,3-amino-5-(4-trifluoromethylbenzyloxy)phenyl, 3-carboxyphenyl,3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl,2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylapinophenyl,2-fluorophenyl, 3-fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl,3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl,phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; Y⁰ isselected from the group consisting of:1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹thiophene, and 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene; R¹⁶ and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl,fluoro, chloro, and cyano; R¹⁶ or R¹⁹ is optionally C(NR²⁵)NR²³R²⁴ withthe proviso that R¹⁶, R¹⁹, and Q^(b) are not simultaneously hydrido; R¹⁷and R¹⁸ are independently selected from the group consisting of hydrido,fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano; Q^(b)is C(NR²⁵)NR²³R²⁴ or hydrido; R²³, R²⁴, and R²⁵ are independentlyhydrido or methyl; Q^(s) is CH₂.
 42. Compound of claim 39 of theFormula:

or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of halo, haloalkyl, hydroxy, hydroxyalkyl,amino, and aminoalkyl; B is a C3-C7 cycloalkyl or a C4-C6 saturatedheterocyclyl, wherein each ring carbon is optionally substituted withR³³, a ring carbon other than the ring carbon at the point of attachmentof B to A is optionally substituted with oxo provided that no more thanone ring carbon is substituted by oxo at the same time, ring carbons anda nitrogen adjacent to the carbon atom at the point of attachment areoptionally substituted with R⁹ or R¹³, a ring carbon or nitrogenadjacent to the R⁹ position and two atoms from the point of attachmentis optionally substituted with R¹⁰, a ring carbon or nitrogen adjacentto the R¹³ position and two atoms from the point of attachment isoptionally substituted with R¹², a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹⁰ position isoptionally substituted with R¹¹, a ring carbon or nitrogen three atomsfrom the point of attachment and adjacent to the R¹² position isoptionally substituted with R³³, and a ring carbon or nitrogen fouratoms from the point of attachment and adjacent to the R¹¹ and R³³positions is optionally substituted with R³⁴; R⁹, R¹¹, and R¹³ areindependently selected from the group consisting of hydrido, hydroxy,amino, amidino, guanidino, alkylamino, alkylthio, alkoxy, alkylsulfinyl,alkylsulfonyl, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy,hydroxyalkyl, carboxy, carboxamido, and cyano; R¹⁰ and R¹² areindependently selected from the group consisting of hydrido, acetamido,haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, hydroxy,amino, alkylamino, alkylsulfonamido, amidosulfonyl, hydroxyalkyl,aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxamido,carboxyalkyl, and cyano; R³³ and R³⁴ are independently selected from thegroup consisting of hydrido, acetamido, haloacetamido, amidino,guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio,amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl,carboalkoxy, carboxy, carboxamido, and cyano; R³³ is optionally Q^(b); Ais a bond or (CH(R¹⁵))_(pa)—(W⁷)_(rr) wherein rr is 0 or 1, pa is aninteger selected from 0 through 3, and W⁷ is N(R⁷); R⁷ is hydrido oralkyl; R¹⁵ is selected from the group consisting of hydrido, halo,alkyl, and haloalkyl; R¹ and X^(o) are independently selected from thegroup consisting of hydrido, hydroxy, hydroxyamino, amidino, amino,cyano, hydroxyalkyl, alkoxy, alkyl, alkylamino, aminoalkyl, alkylthio,alkoxyamino, haloalkyl, haloalkoxy, and halo; R² is Z⁰-Q; Z⁰ is a bond;Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbonadjacent to the carbon at the point of attachment of said phenyl orheteroaryl ring to Z⁰ is optionally substituted by R⁹, the other carbonadjacent to the carbon at the point of attachment is optionallysubstituted by R¹³, a carbon adjacent to R⁹ and two atoms from thecarbon at the point of attachment is optionally substituted by R¹⁰, acarbon adjacent to R¹³ and two atoms from the carbon at the point ofattachment is optionally substituted by R¹², and any carbon adjacent toboth R¹⁰ and R¹² is optionally substituted by R¹¹; Y⁰ is phenyl or aheteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl orsaid heteroaryl is substituted by Q^(s), a carbon two or three atomsfrom the point of attachment of Q^(s) to said phenyl or said heteroarylis substituted by Q^(b), a carbon adjacent to the point of attachment ofQ^(s) is optionally substituted by R¹⁷, another carbon adjacent to thepoint of attachment of Q^(s) is optionally substituted by R¹⁸, a carbonadjacent to Q^(b) is optionally substituted by R¹⁶, and another carbonadjacent to Q^(b) is optionally substituted by R¹⁹; R¹⁶, R¹⁷, R¹⁸, andR¹⁹ are independently selected from the group consisting of hydrido,amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino,alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl,haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl,aminoalkyl, and cyano; R¹⁶ or R¹⁹ is optionally NR²⁰R²¹ orC(NR²⁵)NR²³R²⁴, with the proviso that R¹⁶, R¹⁹, and Q^(b) are notsimultaneously hydrido; Q^(b) is selected from the group consisting ofNR²⁰R²¹, hydrido, and C(NR²⁵)NR²³R²⁴; R²⁰, R²¹, R²³, R²⁴, and R²⁵ areindependently hydrido or alkyl; Q^(s) is CH₂.
 43. Compound of claim 42or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of fluoro, chloro, trifluoromethyl, hydroxy,hydroxymethyl, amino, and aminomethyl; B is selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl,cycloheptyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl,azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, bicyclo[3.1.0]hexan-6-yl,2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl,2-piperazinyl, 1-piperidinyl, 2-piperidinyl, 3-piperidinyl,4-piperidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl,2-dioxanyl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl,2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl,2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein each ring carbonis optionally substituted with R³³, ring carbons and a nitrogen adjacentto the carbon atom at the point of attachment are optionally substitutedwith R⁹ or R¹³, a ring carbon or nitrogen adjacent to the R⁹ positionand two atoms from the point of attachment are optionally substitutedwith R¹⁰, and a ring carbon or nitrogen atom adjacent to the R¹³position and two atoms from the point of attachment is optionallysubstituted with R¹²; R⁹, R¹¹, and R¹³ are independently selected fromthe group consisting of hydrido, methyl, ethyl, methoxy, ethoxy,hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio,trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro,bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl,hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl,carboxy, and cyano; R¹⁰ and R¹² are independently selected from thegroup consisting of hydrido, amidino, amidocarbonyl,N-methylamidocarbonyl, N-benzylamidocarbonyl,N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl,N-(2-trifluoromethylbenzyl)amidocarbonyl,N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl,N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl,N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy,hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy,carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino,dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl,N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro,chloro, bromo, and cyano; R³³ is selected from the group consisting ofhydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy,carboxy, amino, N-methylamino, dimethylamino, methoxyamino, methylthio,ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl,hydroxymethyl, amidocarbonyl, cyano, and Q^(b); A is selected from thegroup consisting of a bond, NH, N(CH₃), CH₂, CH₃CH, CH₂CH₂, andCH₂CH₂CH₂; X^(o) is selected from the group consisting of hydrido,hydroxy, amino, amidino, aminomethyl, cyano, methyl, trifluoromethyl,hydroxymethyl, chloro, and fluoro; R¹ is selected from the groupconsisting of hydrido, hydroxy, hydroxymethyl, amino, aminomethyl,methylamino, cyano, methyl, trifluoromethyl, methoxy, methylthio,trifluoromethoxy, fluoro, and chloro; R² is selected from the groupconsisting of phenyl, 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl,2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl, wherein a carbonadjacent to the carbon at the point of attachment of said phenyl orheteroaryl ring to the benzene ring is optionally substituted by R⁹, theother carbon adjacent to the carbon at the point of attachment isoptionally substituted by R¹³, a carbon adjacent to R⁹ and two atomsfrom the carbon at the point of attachment is optionally substituted byR¹⁰, a carbon adjacent to R¹³ and two atoms from the carbon at the pointof attachment is optionally substituted by R¹², and any carbon adjacentto both R¹⁰ and R¹² is optionally substituted by R¹¹; Y⁰ is selectedfrom the group consisting of: 1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹benzene, 2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene, 3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹pyridine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹ thiophene,3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹ furan, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ furan,3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹ pyrrole, 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷pyrrole, 4-Q^(b)-2-Q^(s)-5-R¹⁹ thiazole, and 2-Q^(b)-5-Q^(s)-4-R¹⁷thiazole; R¹⁶, R¹⁷, R¹⁸, and R¹⁹ are independently selected from thegroup consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy,hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,dimethylamino, methylthio, ethylthio, trifluoromethylthio,methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl,2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl,carboxy, and cyano; Q^(b) is NR²⁰R²¹ or C(NR²⁵)NR²³R²⁴; R²⁰, R²¹, R²³,R²⁴, and R²⁵ are independently selected from the group consisting ofhydrido, methyl, and ethyl; Q^(s) is CH₂.
 44. Compound of claim 43 or apharmaceutically acceptable salt thereof, wherein; J is selected fromthe group consisting of fluoro, trifluoromethyl, hydroxy, hydroxymethyl,amino, and aminomethyl; B is selected from the group consisting ofcyclopropyl, cyclobutyl, cyclopentyl cyclohexyl, oxalan-2-yl,2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl,azetidin-3-yl, 1-pyrrolidinyl and 1-piperidinyl; A is selected from thegroup consisting of a bond, CH₂, CH₂CH₂ and CH₂CH₂CH₂; X^(o) is selectedfrom the group consisting of hydrido, hydroxy, amino, amidino,aminomethyl, cyano, methyl, trifluoromethyl, hydroxymethyl, and fluoro;R¹ is selected from the group consisting of hydrido, hydroxy,hydroxymethyl, amino, aminomethyl, cyano, methyl, trifluoromethyl, andfluoro; R² is selected from the group consisting of3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,3-amino-5-(N-benzylamidocarbonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-benzylamidosulfonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,3-amino-5-(N-ethylamidocarbonyl)phenyl,3-amino-5-(N-isopropylamidocarbonyl)phenyl,3-amino-5-(N-propylamidocarbonyl)phenyl,3-amino-5-(N-isobutylamidocarbonyl)phenyl,3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl,3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl,3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl,2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl,3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl,3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl,2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl,3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl,3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl,5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl,and 3-thienyl; Y⁰ is selected from the group consisting of:1-Q^(b)-4-Q^(s)-2-R¹⁶-3-R¹⁷-5-R¹⁸-6-R¹⁹ benzene,2-Q^(b)-5-Q^(s)-6-R¹⁷-4-R¹⁸-3-R¹⁹ pyridine,3-Q^(b)-6-Q^(s)-2-R¹⁶-5-R¹⁸-4-R¹⁹ pyridine, 3-Q^(b)-5-Q^(s)-4-R¹⁶-2-R¹⁹thiophene, and 2-Q^(b)-5-Q^(s)-3-R¹⁶-4-R¹⁷ thiophene; R¹⁶ and R¹⁹ areindependently selected from the group consisting of hydrido, amidino,amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl,fluoro, chloro, and cyano; R¹⁷ and R¹⁸ are independently selected fromthe group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl,amino, carboxy, and cyano; Q^(b) is C(NR²⁵)NR²³R²⁴; R²³, R²⁴, and R²⁵are independently hydrido or methyl; Q^(s) is CH₂.
 45. Compound of claim44 or a pharmaceutically acceptable salt thereof, wherein; J is selectedfrom the group consisting of fluoro, hydroxy, hydroxymethyl, and amino;B is selected from the group consisting of cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl,oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, and1-piperidinyl; A is selected from the group consisting of a bond, CH₂,CH₂CH₂ and CH₂CH₂CH₂; X^(o) is selected from the group consisting ofhydrido, hydroxy, amino, amidino, aminomethyl, cyano, methyl,trifluoromethyl, hydroxymethyl, and fluoro; R¹ is selected from thegroup consisting of hydrido, hydroxy, hydroxymethyl, amino, aminomethyl,cyano, methyl, trifluoromethyl, and fluoro; R² is selected from thegroup consisting of 3-amidocarbonyl-5-aminophenyl,3-amino-5-(N-benzylamidocarbonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,3-amino-5-(N-benzylamidosulfonyl)phenyl,3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,3-amino-5-(N-ethylamidocarbonyl)phenyl,3-amino-5-(N-isopropylamidocarbonyl)phenyl,3-amino-5-(N-propylamidocarbonyl)phenyl,3-amino-5-(N-isobutylamidocarbonyl)phenyl,3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,3-carboxy-5-aminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl,3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl;Y⁰ is selected from the group consisting of 5-amidino-2-thienylmethyl,4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amdinobenzyl.46. Compound of claim 39 where said compound is selected from the groupof the Formula:

or a pharmaceutically acceptable salt thereof, wherein; R² is3-aminophenyl, B is cyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, Jis hydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is cyclobutyl, A isa bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is 3-aminophenyl, Bis cyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J ishydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is cyclobutyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3-aminophenyl, B is cyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, Jis hydroxy, and R¹ is chloro; R² is 5-amino-2-thienyl, B is cyclobutyl,A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R²is 3-aminophenyl, B is cyclopropyl, A is CH₂, Y⁰ is 4-amidinobenzyl, Jis hydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is2-(2R)-bicyclo[2.2.1]-heptyl, A is a bond, Y⁰ is 4-amidinobenzyl, J ishydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is cyclopentyl, A is abond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R²is 3-aminophenyl, B is cyclohexyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, Jis hydroxy, and R¹ is hydrido; R² is 3-aminophenyl, B is oxalan-2-yl, Ais CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-aminophenyl, B is 1-piperidinyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, Jis hydroxy, and R¹ is chloro; R² is 3-aminophenyl, B is 1-pyrrolidinyl,A is CH₂CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro;R² is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl,J is hydroxy, and R¹ is hydrido; R² is 2-aminocarboxypyridyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ishydrido; R² is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is abond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3,5-diaminophenyl, B is cyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl,J is hydroxy, and R¹ is chloro; R² is 3,5-diaminophenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy,and R¹ is chloro; R² is 3,5-diaminophenyl, B is cyclopropyl, A is abond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R²is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3,5-diaminophenyl, B is cyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl,J is hydroxy, and R¹ is chloro; R² is 3-carboxy-5-aminophenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3-carboxy-5-aminophenyl, B is cyclopentyl, A is a bond, Y⁰ is4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl, A is a bond,Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopentyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclopropyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A isa bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy, and R¹ is chloro;R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy,and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ is hydrido; R² is3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A isa bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is hydroxy, and R¹ is chloro;R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy,and R¹ is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is hydroxy,and R¹ is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ishydrido; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is hydroxy,and R¹ is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is hydroxy, and R¹ ischloro; R² is 3-aminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is 3-aminophenyl, Bis cyclobutyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro,and R¹ is chloro; R² is 3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is 3-aminophenyl,B is cyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J isfluoro, and R¹ is chloro; R² is 3-aminophenyl, B is cyclobutyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is3-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is cyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, Jis fluoro, and R¹ is chloro; R² is 5-amino-2-thienyl, B is cyclobutyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is cyclopropyl, A is CH₂, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is chloro; R² is 3-aminophenyl, B is2-(2R)-bicyclo[2.2.1]-heptyl, A is a bond, Y⁰ is 4-amidinobenzyl, J isfluoro, and R¹ is chloro; R² is 3-aminophenyl, B is cyclopentyl, A is abond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R²is 3-aminophenyl, B is cyclohexyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, Jis fluoro, and R¹ is hydrido; R² is 3-aminophenyl, B is oxalan-2-yl, Ais CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-aminophenyl, B is 1-piperidinyl, A is CH₂CH₂, Y⁰ is 4-amidinobenzyl, Jis fluoro, and R¹ is chloro; R² is 3-aminophenyl, B is 1-pyrrolidinyl, Ais CH₂CH₂CH₂, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R²is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl,J is fluoro, and R¹ is hydrido; R² is 2-amino-6-carboxypyridyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ishydrido; R² is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is 3,5-diaminophenyl,B is cyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, andR¹ is chloro; R² is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3,5-diaminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl,J is fluoro, and R¹ is hydrido; R² is 3,5-diaminophenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is fluoro,and R¹ is chloro; R² is 3,5-diaminophenyl, B is cyclopentyl, A is abond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y⁰ is4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y⁰ is4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-carboxy-5-aminophenyl, B is cyclopentyl, A is a bond, Y⁰ is4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl, A is a bond,Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond,Y⁰ is 4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopentyl, A is a bond,Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclopropyl, Ais a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A isa bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro, and R¹ is chloro;R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro,and R¹ is chloro; R² is3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A isa bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ is hydrido; R² is3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A isa bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is fluoro, and R¹ is chloro;R² is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B iscyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro,and R¹ is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopropyl, A is a bond, Y⁰ is 4-amidino-2-fluorobenzyl, J is fluoro,and R¹ is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ishydrido; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclobutyl, A is a bond, Y⁰ is 4-amidino-3-fluorobenzyl, J is fluoro,and R¹ is chloro; R² is3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B iscyclopentyl, A is a bond, Y⁰ is 4-amidinobenzyl, J is fluoro, and R¹ ischloro.
 47. A composition for inhibiting thrombotic conditions in bloodcomprising a compound of claim 21 and a pharmaceutically acceptablecarrier.
 48. A composition for inhibiting thrombotic conditions in bloodcomprising a compound of claim 21 and a pharmaceutically acceptablecarrier.
 49. A method for inhibiting thrombotic conditions in bloodcomprising adding to blood a therapeutically effective amount of acomposition of claim
 21. 50. A method for inhibiting formation of bloodplatelet aggregates in blood comprising adding to blood atherapeutically effective amount of a composition of claim
 21. 51. Amethod for inhibiting thrombus formation in blood comprising adding toblood a therapeutically effective amount of a composition of claim 21.52. A method for treating or preventing venuous thromboembolism andpulmonary embolism in a mammal comprising administering to the mammal atherapeutically effective amount of a composition of claim
 21. 53. Amethod for treating or preventing deep vein thrombosis in a mammalcomprising administering to the mammal a therapeutically effectiveamount of a composition of claim
 21. 54. A method for treating orpreventing cardiogenic thromboembolism in a mammal comprisingadministering to the mammal a therapeutically effective amount of acomposition of claim
 21. 55. A method for treating or preventingthromboembolic stroke in humans and other mammals comprisingadministering to the mammal a therapeutically effective amount of acomposition of claim
 21. 56. A method for treating or preventingthrombosis associated with cancer and cancer chemotherapy in humans andother mammals comprising administering to the mammal a therapeuticallyeffective amount of a composition of claim
 21. 57. A method for treatingor preventing unstable angina in humans and other mammals comprisingadministering to the mammal a therapeutically effective amount of acomposition of claim
 21. 58. A method for inhibiting thrombus formationin blood comprising adding to blood a therapeutically effective amountof a compound of claim 21 with a therapeutically effective amount offibrinogen receptor antagonist.
 59. The use of a compound of claim 21,or a pharmaceutically acceptable salt thereof, in the manufacture ofmedicament for inhibiting thrombus formation, treating thrombusformation, or preventing thrombus formation in a mammal.